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  2. Protein Tyrosine Kinase/RTK Autophagy Apoptosis
  3. Bcr-Abl Src Autophagy Apoptosis
  4. Dasatinib

Dasatinib  (Synonyms: 達(dá)沙替尼; BMS-354825)

目錄號(hào): HY-10181 純度: 99.88%
COA 產(chǎn)品使用指南

Dasatinib (BMS-354825) 是一種具有口服活性的，ATP 競(jìng)爭(zhēng)性的，雙重 Src/Bcr-Abl 抑制劑，具有有效的抗腫瘤活性。對(duì) Src 和 Bcr-Abl 的 Ki 值分別為 16 pM 和 30 pM。Dasatinib 抑制 Bcr-Abl 和 Src 的IC50 分別為 <1.0 nM 和 0.5 nM。Dasatinib 還誘導(dǎo)凋亡 (apoptosis) 和自噬 (autophagy)。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Dasatinib Chemical Structure

Dasatinib Chemical Structure

CAS No. : 302962-49-8

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥968
In-stock
5 mg ￥233
In-stock
10 mg ￥350
In-stock
50 mg ￥880
In-stock
100 mg ￥1200
In-stock
200 mg ￥1650
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500 mg ￥2400
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1 g   詢價(jià)  
5 g   詢價(jià)  

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Customer Review

Other Forms of Dasatinib:

MCE 顧客使用本產(chǎn)品發(fā)表的 98 篇科研文獻(xiàn)

WB
IF

    Dasatinib purchased from MCE. Usage Cited in: Nat Cell Biol. 2023 Mar;25(3):493-507.  [Abstract]

    Dasatinib (50?nM; 24?or 48?h) significantly decreases MED8A and D458 cell migration.

    Dasatinib purchased from MCE. Usage Cited in: J Hematol Oncol. 2018 Aug 29;11(1):109.  [Abstract]

    YSE450-R and EC109-R cells are treated with 200 nM BIBW 2992 alone or in combination with 100 nM Dasatinib for 48 h.

    Dasatinib purchased from MCE. Usage Cited in: Biol Pharm Bull. 2017;40(10):1747-1753.  [Abstract]

    Synergistic Decrease Bcl-2 Expression by the Combination of SAHA with Dasatinib in MCF-7 Cells.

    Dasatinib purchased from MCE. Usage Cited in: Chem Pharm Bull (Tokyo). 2017 Aug 1;65(8):768-775.  [Abstract]

    Changes in Bcl-2 protein expression in MCF-7 cells after treatment with NSC 105014, Dasatinib or ZD1839 alone or in combination for 12 h. Expression of Bcl-2 protein is analyzed by western blotting analysis.

    Dasatinib purchased from MCE. Usage Cited in: Kawasaki Medical Journal. 43(2)：63-78，2017.

    Western blot analysis of effects of Dasatinib (10 or 100nM) on c-Src, p-SrcY416, FAK and p-FAKY861 expression levels in KTC-1 cells and band intensities for p-SrcY416.

    Dasatinib purchased from MCE. Usage Cited in: Leukemia. 2012 Oct;26(10):2233-44.  [Abstract]

    Drug combination effect on phosphorylation of AKT. Expression of phospho-AKT and total AKT in MOLM13 cells treated for 15 minutes with DMSO vehicle, PKC412 (2.5 nM), Dasatinib (165 nM), or a combination of both. Protein lysates are prepared from MOLM13 cells, and are analyzed via immunoblotting with antibodies to phospho-AKT and total AKT.

    查看 Src 亞型特異性產(chǎn)品:

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively[1]. Dasatinib also induces apoptosis and autophagy.

    IC50 & Target[1]

    Bcr-Abl

    1.0 nM (IC50)

    Src

    0.5 nM (IC50)

    lck

    0.4 nM (IC50)

    yes

    0.5 nM (IC50)

    c-kit

    5.0 nM (IC50)

    PDGFRβ

    28 nM (IC50)

    p38

    100 nM (IC50)

    Her1

    180 nM (IC50)

    Her2

    710 nM (IC50)

    FGFR-1

    880 nM (IC50)

    MEK

    1700 nM (IC50)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A2780 IC50
    8.7 μM
    Compound: 1, Dasatinib
    Cytotoxicity against human A2780 cells after 72 hrs by MTT assay
    Cytotoxicity against human A2780 cells after 72 hrs by MTT assay
    		[PMID: 25815152]
    A549 IC50
    12.66 μM
    Compound: 3
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    		[PMID: 23521020]
    A549 IC50
    23.73 μM
    Compound: Dasatinib
    Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay
    Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay
    		[PMID: 30562697]
    A549 IC50
    8.2 μM
    Compound: Dasatinib, BMS-354825
    Cytotoxicity against human A549 cells after 72 hrs by WST-8 assay
    Cytotoxicity against human A549 cells after 72 hrs by WST-8 assay
    		[PMID: 23567960]
    A549 IC50
    8.37 μM
    Compound: Dasatinib
    Cytotoxicity against human A549 cells assessed as reduction in cell viability after 96 hrs by MTT assay
    Cytotoxicity against human A549 cells assessed as reduction in cell viability after 96 hrs by MTT assay
    		[PMID: 27155464]
    BaF3 GI50
    < 0.0003 μM
    Compound: Dasatinib
    Inhibition of TEL-SRC (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    Inhibition of TEL-SRC (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    BaF3 IC50
    > 1 μM
    Compound: Dasatinib
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay
    		[PMID: 26195136]
    BaF3 EC50
    > 10 μM
    Compound: Dasatinib
    Antiproliferative activity against wild type mouse BA/F3 cells incubated for 3 days by CCK8 assay
    Antiproliferative activity against wild type mouse BA/F3 cells incubated for 3 days by CCK8 assay
    		[PMID: 32657579]
    BaF3 EC50
    > 10 μM
    Compound: Dasatinib
    Protac activity at Cereblon/BCR/ABL T315I mutant (unknown origin) expressed in mouse BaF3 cells assessed as reduction in BCR-ABL T315I mutant driven cell viability incubated for 3 days by CCK8 assay
    Protac activity at Cereblon/BCR/ABL T315I mutant (unknown origin) expressed in mouse BaF3 cells assessed as reduction in BCR-ABL T315I mutant driven cell viability incubated for 3 days by CCK8 assay
    		[PMID: 32657579]
    BaF3 GI50
    > 10 μM
    Compound: Dasatinib
    Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
    Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    BaF3 IC50
    > 100 nM
    Compound: Dasatinib
    Cytotoxicity against mouse BAF3 cells expressing BCR-ABL T315I mutant assessed as inhibition of cell growth measured after 48 hrs by trypan blue assay
    Cytotoxicity against mouse BAF3 cells expressing BCR-ABL T315I mutant assessed as inhibition of cell growth measured after 48 hrs by trypan blue assay
    		[PMID: 34011155]
    BaF3 EC50
    > 1000 nM
    Compound: Dasatinib
    Inhibition of human BCR-ABL T315I mutant expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
    Inhibition of human BCR-ABL T315I mutant expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
    		[PMID: 27010810]
    BaF3 IC50
    0.0002 μM
    Compound: 3
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL M351T mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL M351T mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    		[PMID: 23301703]
    BaF3 IC50
    0.0009 μM
    Compound: 3
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F486S mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F486S mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    		[PMID: 23301703]
    BaF3 GI50
    0.001 μM
    Compound: Dasatinib
    Inhibition of TEL-LCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    Inhibition of TEL-LCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    BaF3 GI50
    0.001 μM
    Compound: Dasatinib
    Inhibition of BCR/ABL p210-Y253F mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    Inhibition of BCR/ABL p210-Y253F mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    BaF3 IC50
    0.0013 μM
    Compound: 3
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E359V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E359V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    		[PMID: 23301703]
    BaF3 IC50
    0.0019 μM
    Compound: 3
    Cytotoxicity against mouse BA/F3 cells expressing wild type BCR-ABL assessed as growth inhibition after 72 hrs by CCK-8 assay
    Cytotoxicity against mouse BA/F3 cells expressing wild type BCR-ABL assessed as growth inhibition after 72 hrs by CCK-8 assay
    		[PMID: 23301703]
    BaF3 IC50
    0.0023 μM
    Compound: 3
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    		[PMID: 23301703]
    BaF3 GI50
    0.003 μM
    Compound: Dasatinib
    Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    BaF3 GI50
    0.003 μM
    Compound: Dasatinib
    Inhibition of BCR/ABL p210-M351T mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    Inhibition of BCR/ABL p210-M351T mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    BaF3 IC50
    0.0032 μM
    Compound: 3
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255K mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255K mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    		[PMID: 23301703]
    BaF3 GI50
    0.004 μM
    Compound: Dasatinib
    Inhibition of BCR/ABL p210-H369P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    Inhibition of BCR/ABL p210-H369P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    BaF3 GI50
    0.005 μM
    Compound: Dasatinib
    Inhibition of TEL-BLK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    Inhibition of TEL-BLK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    BaF3 IC50
    0.0051 μM
    Compound: 3
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL G250E mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL G250E mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    		[PMID: 23301703]
    BaF3 IC50
    0.008 μM
    Compound: 3
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Q252H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Q252H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    		[PMID: 23301703]
    BaF3 GI50
    0.008 μM
    Compound: Dasatinib
    Inhibition of BCR/ABL p210-Q252H mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    Inhibition of BCR/ABL p210-Q252H mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    BaF3 GI50
    0.01 μM
    Compound: Dasatinib
    Inhibition of BCR/ABL p210-F317I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    Inhibition of BCR/ABL p210-F317I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    BaF3 GI50
    0.014 μM
    Compound: Dasatinib
    Inhibition of BCR/ABL p210-F317L mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    Inhibition of BCR/ABL p210-F317L mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    BaF3 IC50
    0.015 μM
    Compound: 3
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E355G mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E355G mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    		[PMID: 23301703]
    BaF3 IC50
    0.017 μM
    Compound: 3
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253F mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253F mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    		[PMID: 23301703]
    BaF3 GI50
    0.017 μM
    Compound: Dasatinib
    Inhibition of BCR/ABL p210-E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    Inhibition of BCR/ABL p210-E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    BaF3 IC50
    0.019 μM
    Compound: 3
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317L mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317L mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    		[PMID: 23301703]
    BaF3 IC50
    0.023 μM
    Compound: 3
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    		[PMID: 23301703]
    BaF3 IC50
    0.025 μM
    Compound: 3
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    		[PMID: 23301703]
    BaF3 IC50
    0.029 μM
    Compound: 3
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL L248V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL L248V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    		[PMID: 23301703]
    BaF3 GI50
    0.039 μM
    Compound: Dasatinib
    Inhibition of TEL-HCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    Inhibition of TEL-HCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    BaF3 EC50
    0.04 nM
    Compound: Dasatinib
    Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
    Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
    		[PMID: 27010810]
    BaF3 IC50
    0.09 μM
    Compound: Dasatinib
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay
    		[PMID: 26814890]
    BaF3 IC50
    0.12 nM
    Compound: 3, BMS-354825
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M244V mutant after 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M244V mutant after 72 hrs by CCK-8 assay
    		[PMID: 23088644]
    BaF3 IC50
    0.31 nM
    Compound: 3, BMS-354825
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396P mutant after 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396P mutant after 72 hrs by CCK-8 assay
    		[PMID: 23088644]
    BaF3 IC50
    0.51 nM
    Compound: 3, BMS-354825
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant after 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant after 72 hrs by CCK-8 assay
    		[PMID: 23088644]
    BaF3 IC50
    0.58 nM
    Compound: 3, BMS-354825
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253F mutant after 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253F mutant after 72 hrs by CCK-8 assay
    		[PMID: 23088644]
    BaF3 IC50
    0.58 nM
    Compound: 3, BMS-354825
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E355G mutant after 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E355G mutant after 72 hrs by CCK-8 assay
    		[PMID: 23088644]
    BaF3 IC50
    0.7 nM
    Compound: Dasatinib
    Cytotoxicity against mouse BAF3 cells expressing native BCR-ABL assessed as inhibition of cell growth measured after 72 hrs by MTT assay
    Cytotoxicity against mouse BAF3 cells expressing native BCR-ABL assessed as inhibition of cell growth measured after 72 hrs by MTT assay
    		[PMID: 34011155]
    BaF3 IC50
    0.83 nM
    Compound: 3, BMS-354825
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant after 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant after 72 hrs by CCK-8 assay
    		[PMID: 23088644]
    BaF3 IC50
    1.29 nM
    Compound: 3, BMS-354825
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant after 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant after 72 hrs by CCK-8 assay
    		[PMID: 23088644]
    BaF3 IC50
    1.71 nM
    Compound: 3, BMS-354825
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F486S mutant after 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F486S mutant after 72 hrs by CCK-8 assay
    		[PMID: 23088644]
    BaF3 IC50
    1.72 nM
    Compound: 3, BMS-354825
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396R mutant after 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396R mutant after 72 hrs by CCK-8 assay
    		[PMID: 23088644]
    BaF3 IC50
    1.91 nM
    Compound: 3, BMS-354825
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant after 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant after 72 hrs by CCK-8 assay
    		[PMID: 23088644]
    BaF3 IC50
    1.94 nM
    Compound: 3, BMS-354825
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F359V mutant after 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F359V mutant after 72 hrs by CCK-8 assay
    		[PMID: 23088644]
    BaF3 IC50
    1714 nM
    Compound: 3, BMS-354825
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay
    		[PMID: 23088644]
    BaF3 IC50
    2.5 μM
    Compound: 3
    Cytotoxicity against mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CCK-8 assay
    Cytotoxicity against mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CCK-8 assay
    		[PMID: 23301703]
    BaF3 GI50
    3 μM
    Compound: Dasatinib
    Inhibition of TEL-DDR1 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    Inhibition of TEL-DDR1 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    BaF3 GI50
    3 μM
    Compound: Dasatinib
    Inhibition of TEL-DDR2 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    Inhibition of TEL-DDR2 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    BaF3 IC50
    3.6 μM
    Compound: 3
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    		[PMID: 23301703]
    BaF3 IC50
    3.8 μM
    Compound: 3
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL H396R mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL H396R mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
    		[PMID: 23301703]
    BaF3 IC50
    4.5 nM
    Compound: 3, BMS-354825
    Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay
    		[PMID: 23088644]
    BaF3 IC50
    5.72 nM
    Compound: 3, BMS-354825
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant after 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant after 72 hrs by CCK-8 assay
    		[PMID: 23088644]
    BaF3 IC50
    6.55 nM
    Compound: 3, BMS-354825
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant after 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant after 72 hrs by CCK-8 assay
    		[PMID: 23088644]
    BaF3 IC50
    6589 nM
    Compound: 3, BMS-354825
    Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CCK-8 assay
    		[PMID: 23088644]
    BaF3 GI50
    9.94 μM
    Compound: Dasatinib
    Inhibition of BCR/ABL p210-T315I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    Inhibition of BCR/ABL p210-T315I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    BXPC-3 EC50
    33 nM
    Compound: Dasatinib
    Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay
    Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay
    		[PMID: 27010810]
    CAKI-2 EC50
    55 nM
    Compound: Dasatinib
    Antiproliferative activity against human Caki2 cells after 72 hrs by MTT assay
    Antiproliferative activity against human Caki2 cells after 72 hrs by MTT assay
    		[PMID: 27010810]
    CHO IC50
    81.1 μM
    Compound: dasatinib
    Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
    Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
    		[PMID: 23812503]
    DLD-1 IC50
    4.6 μM
    Compound: Dasatinib, BMS-354825
    Cytotoxicity against human DLD1 cells after 72 hrs by WST-8 assay
    Cytotoxicity against human DLD1 cells after 72 hrs by WST-8 assay
    		[PMID: 23567960]
    DU-145 GI50
    0.0623 μM
    Compound: Dasatinib
    Antiproliferative activity against human PRXF DU145 cells after 4 days by modified propidium iodide assay
    Antiproliferative activity against human PRXF DU145 cells after 4 days by modified propidium iodide assay
    		[PMID: 25076195]
    DU-145 IC50
    0.0623 μM
    Compound: Dasatinib
    Cytotoxicity against human PRXF DU145 cells after 4 days by propidium iodide staining
    Cytotoxicity against human PRXF DU145 cells after 4 days by propidium iodide staining
    		[PMID: 23253074]
    DU-145 GI50
    0.16 μM
    Compound: Sprycel, NSC 723517
    Cytotoxicity against human DU145 cells after 48 hrs by SRB assay
    Cytotoxicity against human DU145 cells after 48 hrs by SRB assay
    		[PMID: 24015327]
    HCT-116 IC50
    2.3 μM
    Compound: 3
    Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
    		[PMID: 23521020]
    HCT-116 IC50
    3.58 μM
    Compound: Dasatinib
    Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay
    Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay
    		[PMID: 30562697]
    HCT-116 GI50
    3.7 μM
    Compound: Sprycel, NSC 723517
    Cytotoxicity against human HCT116 cells after 48 hrs by SRB assay
    Cytotoxicity against human HCT116 cells after 48 hrs by SRB assay
    		[PMID: 24015327]
    HCT-116 IC50
    5.23 μM
    Compound: Dasatinib
    Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 96 hrs by MTT assay
    Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 96 hrs by MTT assay
    		[PMID: 27155464]
    HCT-116 IC50
    5.3 μM
    Compound: Dasatinib, BMS-354825
    Cytotoxicity against human HCT116 cells after 72 hrs by WST-8 assay
    Cytotoxicity against human HCT116 cells after 72 hrs by WST-8 assay
    		[PMID: 23567960]
    HEK293 EC50
    0.47 μM
    Compound: Dasatinib
    Inhibition of recombinant Nanoluc-tagged p38alpha (unknown origin) expressed in HEK293 cells incubated for 2 to 3 mins by NanoBRET assay
    Inhibition of recombinant Nanoluc-tagged p38alpha (unknown origin) expressed in HEK293 cells incubated for 2 to 3 mins by NanoBRET assay
    		[PMID: 31520926]
    HEK293 IC50
    14.3 μM
    Compound: 1, Dasatinib
    Cytotoxicity against human HEK293 cells after 72 hrs by MTT assay
    Cytotoxicity against human HEK293 cells after 72 hrs by MTT assay
    		[PMID: 25815152]
    HEK293 IC50
    63 nM
    Compound: Dasatinib
    Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells by TR-FRET based binding assay
    Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells by TR-FRET based binding assay
    		[PMID: 22770610]
    HEL GI50
    5.3 μM
    Compound: Dasatinib
    Antiproliferative activity against human HEL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
    Antiproliferative activity against human HEL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    HepG2 IC50
    > 5 μM
    Compound: dasatinib
    Cytotoxicity against human HepG2 cells assessed as cell viability after 72 hrs by MTT assay
    Cytotoxicity against human HepG2 cells assessed as cell viability after 72 hrs by MTT assay
    		[PMID: 25835317]
    HepG2 IC50
    7.5 μM
    Compound: Dasatinib
    Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 27739679]
    HL-60 IC50
    14.97 μM
    Compound: Dasatinib
    Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    		[PMID: 36242991]
    HMEC GI50
    1.8 μM
    Compound: Sprycel, NSC 723517
    Cytotoxicity against human HMEC after 72 hrs by WST1 assay
    Cytotoxicity against human HMEC after 72 hrs by WST1 assay
    		[PMID: 24015327]
    Hs-578T GI50
    0.03 μM
    Compound: Sprycel, NSC 723517
    Cytotoxicity against human Hs578T cells after 48 hrs by SRB assay
    Cytotoxicity against human Hs578T cells after 48 hrs by SRB assay
    		[PMID: 24015327]
    JeKo-1 IC50
    1325 nM
    Compound: Dasatinib
    Growth inhibition of human Jeko-1 cells incubated for 72 hrs
    Growth inhibition of human Jeko-1 cells incubated for 72 hrs
    		[PMID: 33479666]
    Jurkat IC50
    > 1000 nM
    Compound: Dasatinib
    Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
    Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
    		[PMID: 34011155]
    K562 GI50
    < 0.0003 μM
    Compound: Dasatinib
    Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
    Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    K562 IC50
    < 1 nM
    Compound: 13, BMS-354825
    Antiproliferative activity against human K562 cells after 72 hrs
    Antiproliferative activity against human K562 cells after 72 hrs
    		[PMID: 15615512]
    K562 IC50
    0.00025 μM
    Compound: Dasatinib
    Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay
    Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay
    		[PMID: 26814890]
    K562 GI50
    0.0004 μM
    Compound: BMS-354825
    Growth inhibition of human K562 cells measured after 48 hrs by alamarblue assay
    Growth inhibition of human K562 cells measured after 48 hrs by alamarblue assay
    		[PMID: 35944901]
    K562 IC50
    0.000638 μM
    Compound: 3
    Antiproliferative activity against human K562 cells assessed as reduction in cell viability by measuring ATP level incubated for 3 days by Celltiter-Glo assay
    Antiproliferative activity against human K562 cells assessed as reduction in cell viability by measuring ATP level incubated for 3 days by Celltiter-Glo assay
    		[PMID: 31303996]
    K562 IC50
    0.0007 μM
    Compound: 3
    Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay
    		[PMID: 23521020]
    K562 IC50
    0.001 μM
    Compound: Dasatinib
    Antiproliferative activity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    		[PMID: 36242991]
    K562 IC50
    0.001 μM
    Compound: Dasatinib
    Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay
    Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay
    		[PMID: 26195136]
    K562 IC50
    0.19 nM
    Compound: Dasatinib
    Antiproliferative activity against human K562 cells incubated for 3 days by CCK8 assay
    Antiproliferative activity against human K562 cells incubated for 3 days by CCK8 assay
    		[PMID: 32657579]
    K562 IC50
    0.2 nM
    Compound: Dasatinib
    Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
    Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
    		[PMID: 34011155]
    K562 CC50
    0.25 μM
    Compound: VI
    Cytotoxicity against human K562 cells assessed as decrease in cell viability by MTT assay
    Cytotoxicity against human K562 cells assessed as decrease in cell viability by MTT assay
    		[PMID: 27474918]
    K562 IC50
    0.45 μM
    Compound: BMS-354825
    Cytotoxicity against human K562 cells expressing Bcr-Abl assessed as growth inhibition after 48 hrs by MTT assay
    Cytotoxicity against human K562 cells expressing Bcr-Abl assessed as growth inhibition after 48 hrs by MTT assay
    		[PMID: 26451772]
    K562 IC50
    0.9 nM
    Compound: Dasatinib
    Growth inhibition of human K562 cells incubated for 2 days by CCK8 assay
    Growth inhibition of human K562 cells incubated for 2 days by CCK8 assay
    		[PMID: 31539241]
    K562 IC50
    0.9 nM
    Compound: Dasatinib
    Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay
    		[PMID: 34217059]
    K562 IC50
    1 nM
    Compound: 2, dasatinib,BMS-354825
    Growth inhibition of human K562 cells after 48 hrs by [3H]thymidine uptake assay
    Growth inhibition of human K562 cells after 48 hrs by [3H]thymidine uptake assay
    		[PMID: 17956080]
    K562 IC50
    11.9 μM
    Compound: Dasatinib, BMS-354825
    Cytotoxicity against human K562 cells after 72 hrs by WST-8 assay
    Cytotoxicity against human K562 cells after 72 hrs by WST-8 assay
    		[PMID: 23567960]
    K562 IC50
    11.95 μM
    Compound: Dasatinib
    Cytotoxicity against human K562 cells assessed as reduction in cell viability after 96 hrs by MTT assay
    Cytotoxicity against human K562 cells assessed as reduction in cell viability after 96 hrs by MTT assay
    		[PMID: 27155464]
    K562 IC50
    12.83 μM
    Compound: BMS-354825, SPRYCEL
    Cytotoxicity against human K562 cells after 72 hrs by WST-8 reagent based MTT assay
    Cytotoxicity against human K562 cells after 72 hrs by WST-8 reagent based MTT assay
    		[PMID: 22217877]
    K562 GI50
    9.7 μM
    Compound: BMS-354825
    Growth inhibition of human K562 cells expressing BCR-ABL T315I mutant measured after 48 hrs by alamarblue assay
    Growth inhibition of human K562 cells expressing BCR-ABL T315I mutant measured after 48 hrs by alamarblue assay
    		[PMID: 35944901]
    KM12 GI50
    7.44 μM
    Compound: Sprycel, NSC 723517
    Cytotoxicity against human KM12 cells after 48 hrs by SRB assay
    Cytotoxicity against human KM12 cells after 48 hrs by SRB assay
    		[PMID: 24015327]
    KU812 cell line GI50
    < 0.0003 μM
    Compound: Dasatinib
    Antiproliferative activity against human KU812 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
    Antiproliferative activity against human KU812 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    KU812 cell line IC50
    0.1 nM
    Compound: Dasatinib
    Cytotoxicity against human KU812 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
    Cytotoxicity against human KU812 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
    		[PMID: 34011155]
    L02 IC50
    > 40 μM
    Compound: Dasatinib
    Cytotoxicity against human L02 cells assessed as reduction in cell viability after 96 hrs by MTT assay
    Cytotoxicity against human L02 cells assessed as reduction in cell viability after 96 hrs by MTT assay
    		[PMID: 27155464]
    Malme-3M GI50
    6.61 μM
    Compound: Sprycel, NSC 723517
    Cytotoxicity against human MALME-3M cells after 48 hrs by SRB assay
    Cytotoxicity against human MALME-3M cells after 48 hrs by SRB assay
    		[PMID: 24015327]
    Maver1 IC50
    1325 nM
    Compound: Dasatinib
    Growth inhibition of human MAVER-1 cells incubated for 72 hrs
    Growth inhibition of human MAVER-1 cells incubated for 72 hrs
    		[PMID: 33479666]
    MCF7 IC50
    1.11 μM
    Compound: Dasatinib
    Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay
    Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay
    		[PMID: 30562697]
    MCF7 IC50
    2.57 μM
    Compound: 3
    Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
    		[PMID: 23521020]
    MCF7 IC50
    8.05 μM
    Compound: 1a
    Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay
    Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay
    		[PMID: 25899332]
    MCF7 GI50
    8.32 μM
    Compound: Sprycel, NSC 723517
    Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay
    Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay
    		[PMID: 24015327]
    MDA-MB-231 GI50
    0.02 μM
    Compound: Sprycel, NSC 723517
    Cytotoxicity against human MDA-MB-231 cells after 48 hrs by SRB assay
    Cytotoxicity against human MDA-MB-231 cells after 48 hrs by SRB assay
    		[PMID: 24015327]
    MDA-MB-231 IC50
    0.112 μM
    Compound: Dasatinib
    Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 27739679]
    MDA-MB-231 IC50
    0.178 μM
    Compound: dasatinib
    Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay
    		[PMID: 25835317]
    MDA-MB-231 IC50
    1.12 μM
    Compound: 1a
    Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay
    Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay
    		[PMID: 25899332]
    MDA-MB-231 IC50
    12 nM
    Compound: 13, BMS-354825
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs
    		[PMID: 15615512]
    MDA-MB-231 EC50
    44 nM
    Compound: Dasatinib
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
    		[PMID: 27010810]
    MDA-MB-435 IC50
    5.147 μM
    Compound: Dasatinib
    Antiproliferative activity against human MDA-MB-435 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-435 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 27739679]
    MDA-MB-435S IC50
    3.9 μM
    Compound: 3
    Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay
    		[PMID: 23521020]
    MEG-01 GI50
    < 0.0003 μM
    Compound: Dasatinib
    Antiproliferative activity against human MEG01 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
    Antiproliferative activity against human MEG01 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    MOLM-14 GI50
    2.3 μM
    Compound: Dasatinib
    Antiproliferative activity against human MOLM14 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
    Antiproliferative activity against human MOLM14 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    MV4-11 GI50
    3.6 μM
    Compound: Dasatinib
    Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
    Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    NCI-H1975 EC50
    173 nM
    Compound: Dasatinib
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay
    		[PMID: 27010810]
    NCI-H2286 IC50
    0.032 μM
    Compound: Dasatinib
    Antiproliferative activity against human NCI-H2286 cells expressing DDR2 mutant after 72 hrs by alamar blue assay
    Antiproliferative activity against human NCI-H2286 cells expressing DDR2 mutant after 72 hrs by alamar blue assay
    		[PMID: 26191369]
    NCI-H2286 IC50
    33.3 nM
    Compound: Dasatinib
    Antiproliferative activity against human NCI-H2286 cells harboring DDR2 mutation after 72 hrs by CCK8 assay
    Antiproliferative activity against human NCI-H2286 cells harboring DDR2 mutation after 72 hrs by CCK8 assay
    		[PMID: 30572178]
    NCI-H23 IC50
    2.27 μM
    Compound: 3
    Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay
    		[PMID: 23521020]
    NCI-H460 IC50
    8.99 μM
    Compound: 3
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay
    		[PMID: 23521020]
    NCI-H661 IC50
    7.8 μM
    Compound: Dasatinib, BMS-354825
    Cytotoxicity against human NCI-H661 cells after 72 hrs by WST-8 assay
    Cytotoxicity against human NCI-H661 cells after 72 hrs by WST-8 assay
    		[PMID: 23567960]
    NHDF IC50
    0.71 μM
    Compound: Dasatinib
    Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay
    Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay
    		[PMID: 30562697]
    PC-3 EC50
    232 nM
    Compound: Dasatinib
    Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
    Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
    		[PMID: 27010810]
    PC-3 IC50
    9.4 nM
    Compound: 13, BMS-354825
    Antiproliferative activity against human PC3 cells after 72 hrs
    Antiproliferative activity against human PC3 cells after 72 hrs
    		[PMID: 15615512]
    SW-620 GI50
    8.43 μM
    Compound: Sprycel, NSC 723517
    Cytotoxicity against human SW620 cells after 48 hrs by SRB assay
    Cytotoxicity against human SW620 cells after 48 hrs by SRB assay
    		[PMID: 24015327]
    T47D IC50
    0.9 μM
    Compound: 3
    Antiproliferative activity against human T47D cells after 72 hrs by MTT assay
    Antiproliferative activity against human T47D cells after 72 hrs by MTT assay
    		[PMID: 23521020]
    U-251 GI50
    2.81 μM
    Compound: Sprycel, NSC 723517
    Cytotoxicity against human U251 cells after 48 hrs by SRB assay
    Cytotoxicity against human U251 cells after 48 hrs by SRB assay
    		[PMID: 24015327]
    U-937 GI50
    > 10 μM
    Compound: Dasatinib
    Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
    Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
    		[PMID: 26789553]
    U-937 IC50
    > 1000 nM
    Compound: Dasatinib
    Cytotoxicity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
    Cytotoxicity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
    		[PMID: 34011155]
    U-937 IC50
    ≥ 100 nM
    Compound: dasatinib
    Inhibition of LPS-induced Btk autophosphorylation on Tyr223 in human U937 cells at >= 100 nM after 1 hr
    Inhibition of LPS-induced Btk autophosphorylation on Tyr223 in human U937 cells at >= 100 nM after 1 hr
    		[PMID: 17684099]
    U-937 IC50
    10.23 μM
    Compound: Dasatinib
    Cytotoxicity against human U937 cells assessed as reduction in cell viability after 96 hrs by MTT assay
    Cytotoxicity against human U937 cells assessed as reduction in cell viability after 96 hrs by MTT assay
    		[PMID: 27155464]
    U-937 IC50
    12.2 μM
    Compound: Dasatinib, BMS-354825
    Cytotoxicity against human U937 cells after 72 hrs by WST-8 assay
    Cytotoxicity against human U937 cells after 72 hrs by WST-8 assay
    		[PMID: 23567960]
    U-937 IC50
    13.63 μM
    Compound: BMS-354825, SPRYCEL
    Cytotoxicity against human U937 cells after 72 hrs by WST-8 reagent based MTT assay
    Cytotoxicity against human U937 cells after 72 hrs by WST-8 reagent based MTT assay
    		[PMID: 22217877]
    U-937 IC50
    15.02 μM
    Compound: Dasatinib
    Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    		[PMID: 36242991]
    WiDr IC50
    52 nM
    Compound: 13, BMS-354825
    Antiproliferative activity against human WiDr cells after 72 hrs
    Antiproliferative activity against human WiDr cells after 72 hrs
    		[PMID: 15615512]
    體外研究
    (In Vitro)

    Dasatinib 對(duì) Bcr-Abl、Src、Lck、Yes、c-Kit、PDGFRβ、p38、Her1、Her2、FGFR-1 和 MEK 具有顯著活性，IC50<1.0、0.50、分別為 0.40、0.50、5.0、28、100、180、720、880 和 1700 nM[1]。
    與 K562 慢性粒細(xì)胞白血病 (CML)、PC3 相比，Dasatinib 顯示出抗增殖活性人前列腺腫瘤、MDA-MB-231 人乳腺腫瘤和 WiDr 人結(jié)腸腫瘤細(xì)胞系，IC50 分別為 <1.0 nM、9.4 nM、12 nM 和 52 nM[1]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    Dasatinib (5 mg/kg 和 50 mg/kg，qd×10d，5 on-2 off) 在慢性粒細(xì)胞白血病 (CML) 的 K562 異種移植模型中具有有效的抗腫瘤活性和高安全邊際，表明腫瘤完全消退且低多劑量水平的毒性[1]。
    Dasatinib (10 mg/kg) 的藥代動(dòng)力學(xué)特征適合繼續(xù)推進(jìn)體內(nèi)藥效研究。Dasatinib (10 mg/kg) 在靜脈注射和口服時(shí)表現(xiàn)出良好的半衰期 (t1/2s)，分別為 3.3 和 3.1 小時(shí)。本研究口服生物利用度 (Fpo) 為 27%[1]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Nude mice bearing K562 xenografts
    Dosage: 5 mg/kg and 50 mg/kg
    Administration: Oral administration on a 5 day on and 2 day off schedule.
    Result: Showed partial tumor regressions after one treatment cycle and complete disappearance of the tumor mass by the end of drug treatment. No toxicity (animal deaths, lack of weight gain) was observed.
    Animal Model: Sprague-Dawley Rats
    Dosage: 10 mg/kg (Pharmacokinetic Analysis)
    Administration: Oral and i.v.
    Result: Cmax of 13.2 and 0.5 μM for i.v. and oral, respectively.
    Clinical Trial
    分子量

    488.01

    Formula

    C22H26ClN7O2S
    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    中文名稱(chēng)

    達(dá)沙替尼
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : 125 mg/mL (256.14 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.0491 mL 10.2457 mL 20.4914 mL
    5 mM 0.4098 mL 2.0491 mL 4.0983 mL
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動(dòng)物實(shí)驗(yàn)：

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

    • 方案 一

      請(qǐng)依序添加每種溶劑： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.5 mg/mL (5.12 mM); 澄清溶液

    • 方案 二

      請(qǐng)依序添加每種溶劑： 5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.12 mM); 澄清溶液

    以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶。

    • 方案 一

      請(qǐng)依序添加每種溶劑： 0.5% CMC-Na/saline water

      Solubility: 50 mg/mL (102.46 mM); 懸濁液; 超聲助溶

    • 方案 二

      請(qǐng)依序添加每種溶劑： 20% SBE-β-CD in Saline

      Solubility: 2 mg/mL (4.10 mM); 懸濁液; 超聲助溶

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.88%

    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0491 mL 10.2457 mL 20.4914 mL 51.2285 mL
    5 mM 0.4098 mL 2.0491 mL 4.0983 mL 10.2457 mL
    10 mM 0.2049 mL 1.0246 mL 2.0491 mL 5.1228 mL
    15 mM 0.1366 mL 0.6830 mL 1.3661 mL 3.4152 mL
    20 mM 0.1025 mL 0.5123 mL 1.0246 mL 2.5614 mL
    25 mM 0.0820 mL 0.4098 mL 0.8197 mL 2.0491 mL
    30 mM 0.0683 mL 0.3415 mL 0.6830 mL 1.7076 mL
    40 mM 0.0512 mL 0.2561 mL 0.5123 mL 1.2807 mL
    50 mM 0.0410 mL 0.2049 mL 0.4098 mL 1.0246 mL
    60 mM 0.0342 mL 0.1708 mL 0.3415 mL 0.8538 mL
    80 mM 0.0256 mL 0.1281 mL 0.2561 mL 0.6404 mL
    100 mM 0.0205 mL 0.1025 mL 0.2049 mL 0.5123 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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