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  1. Vitamin D Related/Nuclear Receptor Autophagy
  2. Androgen Receptor Autophagy
  3. Bicalutamide

Bicalutamide  (Synonyms: 比卡魯胺)

目錄號: HY-14249 純度: 99.85%
COA 產(chǎn)品使用指南

Bicalutamide 是一種具有口服活性的非甾體雄激素受體 (AR) 拮抗劑。Bicalutamide 可用于前列腺癌的研究。

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)

Bicalutamide Chemical Structure

Bicalutamide Chemical Structure

CAS No. : 90357-06-5

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Customer Review

Other Forms of Bicalutamide:

    Bicalutamide purchased from MCE. Usage Cited in: Sci Rep. 2017 Jun 8;7(1):3058.  [Abstract]

    CXCR7 mRNA in cells treated with 2?μM Bicalutamide (BiC) relative to untreated (UT) cells.
    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer[1].

    IC50 & Target

    Androgen receptor[1]

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    CHO-K1 IC50
    200 nM
    Compound: 3
    Displacement of [3H]mibolerone from human AR expressed in CHO-K1 cells after 2 hrs by scintillation counting
    Displacement of [3H]mibolerone from human AR expressed in CHO-K1 cells after 2 hrs by scintillation counting
    [PMID: 20381361]
    COS-1 IC50
    8.69 x 10-2 μM
    Compound: Bic
    Antagonist activity against pSG5-tagged human androgen receptor expressed in COS1 cells assessed as reduction in receptor-mediated transcriptional activity by AR-regulated rat probasin promoter fragment driven firefly luciferase reporter assay
    Antagonist activity against pSG5-tagged human androgen receptor expressed in COS1 cells assessed as reduction in receptor-mediated transcriptional activity by AR-regulated rat probasin promoter fragment driven firefly luciferase reporter assay
    [PMID: 25646649]
    COS-7 EC50
    > 10 μM
    Compound: Bicalutamide
    Agonist activity at androgen receptor expressed in Cos7 cells after 24 hrs by luciferase reporter gene assay
    Agonist activity at androgen receptor expressed in Cos7 cells after 24 hrs by luciferase reporter gene assay
    [PMID: 22391033]
    COS-7 EC50
    > 10 μM
    Compound: Bicalutamide
    Agonist activity at androgen receptor T877A mutant expressed in Cos7 cells after 24 hrs by luciferase reporter gene assay
    Agonist activity at androgen receptor T877A mutant expressed in Cos7 cells after 24 hrs by luciferase reporter gene assay
    [PMID: 22391033]
    COS-7 IC50
    > 10 μM
    Compound: Bicalutamide
    Antagonist activity at human androgen receptor W741C mutant expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by reporter gene assay
    Antagonist activity at human androgen receptor W741C mutant expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by reporter gene assay
    [PMID: 22094279]
    COS-7 EC50
    > 10 μM
    Compound: Bicalutamide
    Agonist activity at human androgen receptor expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay
    Agonist activity at human androgen receptor expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay
    [PMID: 22094279]
    COS-7 EC50
    > 10 μM
    Compound: Bicalutamide
    Agonist activity at human androgen receptor T877A mutant expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay
    Agonist activity at human androgen receptor T877A mutant expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay
    [PMID: 22094279]
    COS-7 EC50
    0.18 μM
    Compound: Bicalutamide
    Agonist activity at human androgen receptor W741C mutant expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay
    Agonist activity at human androgen receptor W741C mutant expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay
    [PMID: 22094279]
    COS-7 IC50
    0.33 μM
    Compound: Bicalutamide
    Antagonist activity at androgen receptor expressed in Cos7 cells assessed as inhibition of dihydrotestosterone-induced luciferase activity after 24 hrs by reporter gene assay
    Antagonist activity at androgen receptor expressed in Cos7 cells assessed as inhibition of dihydrotestosterone-induced luciferase activity after 24 hrs by reporter gene assay
    [PMID: 22391033]
    COS-7 IC50
    0.33 μM
    Compound: Bicalutamide
    Antagonist activity at human androgen receptor expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by reporter gene assay
    Antagonist activity at human androgen receptor expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by reporter gene assay
    [PMID: 22094279]
    COS-7 IC50
    0.33 μM
    Compound: Bicalutamide
    Antagonist activity at wild type Androgen receptor (unknown origin) expressed in human Cos-7 cells co-expressing pGL3-MMTV-luc vector assessed as luciferase activity by reporter gene assay
    Antagonist activity at wild type Androgen receptor (unknown origin) expressed in human Cos-7 cells co-expressing pGL3-MMTV-luc vector assessed as luciferase activity by reporter gene assay
    [PMID: 23199477]
    COS-7 IC50
    0.47 μM
    Compound: Bicalutamide
    Antagonist activity at androgen receptor T877A mutant expressed in Cos7 cells assessed as inhibition of dihydrotestosterone-induced luciferase activity after 24 hrs by reporter gene assay
    Antagonist activity at androgen receptor T877A mutant expressed in Cos7 cells assessed as inhibition of dihydrotestosterone-induced luciferase activity after 24 hrs by reporter gene assay
    [PMID: 22391033]
    COS-7 IC50
    0.47 μM
    Compound: Bicalutamide
    Antagonist activity at human androgen receptor T877A mutant expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by reporter gene assay
    Antagonist activity at human androgen receptor T877A mutant expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by reporter gene assay
    [PMID: 22094279]
    COS-7 IC50
    0.47 μM
    Compound: Bicalutamide
    Antagonist activity at Androgen receptor T877A mutant (unknown origin) expressed in human Cos-7 cells co-expressing pGL3-MMTV-luc vector assessed as luciferase activity by reporter gene assay
    Antagonist activity at Androgen receptor T877A mutant (unknown origin) expressed in human Cos-7 cells co-expressing pGL3-MMTV-luc vector assessed as luciferase activity by reporter gene assay
    [PMID: 23199477]
    CV-1 EC50
    > 10000 nM
    Compound: Bicalutamide
    Agonist activity at human androgen receptor african green monkey CV1 cells by cotransfection assay
    Agonist activity at human androgen receptor african green monkey CV1 cells by cotransfection assay
    [PMID: 18442912]
    CV-1 IC50
    0.3 μM
    Compound: Casodex
    Antagonist activity at human androgen receptor expressed in human CV1 cells assessed as inhibition of receptor-mediated transactivation by MMTV-luciferase reporter gene assay
    Antagonist activity at human androgen receptor expressed in human CV1 cells assessed as inhibition of receptor-mediated transactivation by MMTV-luciferase reporter gene assay
    [PMID: 20826091]
    CV-1 IC50
    162 nM
    Compound: Bicalutamide
    Antagonist activity at human androgen receptor african green monkey CV1 cells by cotransfection assay
    Antagonist activity at human androgen receptor african green monkey CV1 cells by cotransfection assay
    [PMID: 18442912]
    CV-1 IC50
    162 nM
    Compound: bicalutamide
    Antagonist activity at human androgen receptor in CV1 cells by transcriptional activation assay
    Antagonist activity at human androgen receptor in CV1 cells by transcriptional activation assay
    [PMID: 18400499]
    CWR22R GI50
    3.81 μM
    Compound: Casodex
    Growth inhibition of human CWR22Rv1 cells by MTT assay
    Growth inhibition of human CWR22Rv1 cells by MTT assay
    [PMID: 25634130]
    CWR22R IC50
    4.6 μM
    Compound: 4
    Antagonist activity at androgen receptor H874Y mutant (unknown origin) expressed in human 22Rv1 cells assessed as inhibition of DHT-induced cell growth after 3 days by WST-8 assay
    Antagonist activity at androgen receptor H874Y mutant (unknown origin) expressed in human 22Rv1 cells assessed as inhibition of DHT-induced cell growth after 3 days by WST-8 assay
    [PMID: 24900588]
    CWR22R IC50
    46.25 μM
    Compound: Bicalutamide
    Antiproliferative activity against human 22Rv1 cells after 96 hrs by Oncotest monolayer assay
    Antiproliferative activity against human 22Rv1 cells after 96 hrs by Oncotest monolayer assay
    [PMID: 26965862]
    CWR22R IC50
    48.49 μM
    Compound: 3; Casodex; Bicalutamide
    Antiproliferative activity against human 22Rv1 cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay
    Antiproliferative activity against human 22Rv1 cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay
    [PMID: 27131065]
    CWR22R IC50
    49.577 μM
    Compound: 3; Casodex; Bicalutamide
    Antiproliferative activity against human 22Rv1 cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay
    Antiproliferative activity against human 22Rv1 cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay
    [PMID: 27131065]
    CWR22R IC50
    49.58 μM
    Compound: RS-Bicalutamide
    Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay
    Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay
    [PMID: 27301368]
    CWR22R IC50
    49.6 μM
    Compound: 1
    Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay
    Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay
    [PMID: 31288149]
    DU-145 IC50
    18 μM
    Compound: Bicalutamide
    Cytotoxicity against ERalpha-deficient human DU145 cells expressing ERbeta assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against ERalpha-deficient human DU145 cells expressing ERbeta assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 23786452]
    DU-145 IC50
    46.031 μM
    Compound: 3; Casodex; Bicalutamide
    Antiproliferative activity against human DU145 cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay
    Antiproliferative activity against human DU145 cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay
    [PMID: 27131065]
    DU-145 IC50
    49.2 μM
    Compound: 1
    Antiproliferative activity against human DU145 cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay
    Antiproliferative activity against human DU145 cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay
    [PMID: 31288149]
    DU-145 IC50
    49.2 μM
    Compound: RS-Bicalutamide
    Antiproliferative activity against human DU145 cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay
    Antiproliferative activity against human DU145 cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay
    [PMID: 27301368]
    DU-145 IC50
    49.2 μM
    Compound: 3; Casodex; Bicalutamide
    Antiproliferative activity against human DU145 cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay
    Antiproliferative activity against human DU145 cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay
    [PMID: 27131065]
    DU-145 IC50
    64 μM
    Compound: Casodex
    Cytotoxicity against human androgen-independent DU145 cells by MTT assay
    Cytotoxicity against human androgen-independent DU145 cells by MTT assay
    [PMID: 22326399]
    HEK293 IC50
    0.054 μM
    Compound: Bicalutamide
    Displacement of [17-alpha-methyl-3H]mibolerone from androgen receptor expressed in HEK293 cells after 3 hrs
    Displacement of [17-alpha-methyl-3H]mibolerone from androgen receptor expressed in HEK293 cells after 3 hrs
    [PMID: 22391033]
    HEK293 IC50
    0.054 μM
    Compound: Bicalutamide
    Displacement of [17-alpha-methyl-3H]-mibolerone from human androgen receptor expressed in HEK293 derived FreeStyle293F cells after 3 hrs
    Displacement of [17-alpha-methyl-3H]-mibolerone from human androgen receptor expressed in HEK293 derived FreeStyle293F cells after 3 hrs
    [PMID: 22094279]
    HEK293 IC50
    0.12 μM
    Compound: Bicalutamide
    Displacement of [17-alpha-methyl-3H]mibolerone from androgen receptor T877A mutant expressed in HEK293 cells after 3 hrs
    Displacement of [17-alpha-methyl-3H]mibolerone from androgen receptor T877A mutant expressed in HEK293 cells after 3 hrs
    [PMID: 22391033]
    HEK293 IC50
    0.12 μM
    Compound: Bicalutamide
    Displacement of [17-alpha-methyl-3H]-mibolerone from human androgen receptor T877A mutant expressed in HEK293 derived FreeStyle293F cells after 3 hrs
    Displacement of [17-alpha-methyl-3H]-mibolerone from human androgen receptor T877A mutant expressed in HEK293 derived FreeStyle293F cells after 3 hrs
    [PMID: 22094279]
    HeLa IC50
    140 nM
    Compound: 3
    Antagonist activity at human androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone induced transcriptional activity by reporter gene assay
    Antagonist activity at human androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone induced transcriptional activity by reporter gene assay
    [PMID: 17804229]
    HeLa IC50
    140 nM
    Compound: 3
    Antagonist activity at androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone-induced transcriptional activity by reporter gene assay
    Antagonist activity at androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone-induced transcriptional activity by reporter gene assay
    [PMID: 17064916]
    HeLa IC50
    200 nM
    Compound: 3
    Antagonist activity at human AR expressed in human HeLa cells co-transfected with MMTV-Luc-Hyg after 48 hrs by transient-luciferase reporter gene assay
    Antagonist activity at human AR expressed in human HeLa cells co-transfected with MMTV-Luc-Hyg after 48 hrs by transient-luciferase reporter gene assay
    [PMID: 21050768]
    LNCaP IC50
    > 100 μM
    Compound: Casodex
    Inhibition of BF3 site of androgen receptor in enzalutamide-resistant human LNCAP cells assessed as reduction in PSA level after 3 days
    Inhibition of BF3 site of androgen receptor in enzalutamide-resistant human LNCAP cells assessed as reduction in PSA level after 3 days
    [PMID: 23301637]
    LNCaP IC50
    0.27 μM
    Compound: Bicalutamide
    Inhibition of androgen receptor in human LNCAP cells after 1 day by luciferase reporter gene assay
    Inhibition of androgen receptor in human LNCAP cells after 1 day by luciferase reporter gene assay
    [PMID: 23727044]
    LNCaP IC50
    0.94 μM
    Compound: 4
    Antagonist activity at androgen receptor T877A mutant (unknown origin) expressed in human LNCAP cells assessed as inhibition of DHT-induced cell growth after 6 days by WST-8 assay
    Antagonist activity at androgen receptor T877A mutant (unknown origin) expressed in human LNCAP cells assessed as inhibition of DHT-induced cell growth after 6 days by WST-8 assay
    [PMID: 24900588]
    LNCaP EC50
    1.4 μM
    Compound: 2
    Displacement of [3H]R1881 from AR in human LNCaP cells after 2 hrs by scintillation counting analysis
    Displacement of [3H]R1881 from AR in human LNCaP cells after 2 hrs by scintillation counting analysis
    [PMID: 23713567]
    LNCaP IC50
    1.71 μM
    Compound: Casodex
    Cytotoxicity against human androgen-dependent LNCAP cells by MTT assay
    Cytotoxicity against human androgen-dependent LNCAP cells by MTT assay
    [PMID: 22326399]
    LNCaP IC50
    2.38 μM
    Compound: BIC
    Cytotoxicity against human LNCAP cells assessed as reduction in cell viability after 4 days by MTT assay in presence of DHT and E2
    Cytotoxicity against human LNCAP cells assessed as reduction in cell viability after 4 days by MTT assay in presence of DHT and E2
    [PMID: 26780832]
    LNCaP GI50
    2.61 μM
    Compound: Casodex
    Growth inhibition of human LNCAP cells by MTT assay
    Growth inhibition of human LNCAP cells by MTT assay
    [PMID: 25634130]
    LNCaP IC50
    23.79 μM
    Compound: Bicalutamide
    Cytotoxicity against human LNCAP cells assessed as cell viability after 2 days by cell counting method
    Cytotoxicity against human LNCAP cells assessed as cell viability after 2 days by cell counting method
    [PMID: 23727044]
    LNCaP IC50
    400 nM
    Compound: 5
    Antagonist activity at wild type human AR expressed in human LNCAP cells by transactivation assay
    Antagonist activity at wild type human AR expressed in human LNCAP cells by transactivation assay
    [PMID: 20584610]
    LNCaP IC50
    45.269 μM
    Compound: 3; Casodex; Bicalutamide
    Antiproliferative activity against human LNCAP cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay
    Antiproliferative activity against human LNCAP cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay
    [PMID: 27131065]
    LNCaP IC50
    45.27 μM
    Compound: RS-Bicalutamide
    Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay
    Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay
    [PMID: 27301368]
    LNCaP IC50
    45.3 μM
    Compound: 1
    Antiproliferative activity against human LNCAP cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay
    Antiproliferative activity against human LNCAP cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay
    [PMID: 31288149]
    LNCaP IC50
    47.266 μM
    Compound: 3; Casodex; Bicalutamide
    Antiproliferative activity against human LNCAP cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay
    Antiproliferative activity against human LNCAP cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay
    [PMID: 27131065]
    LNCaP IC50
    550 nM
    Compound: 3
    Antagonist activity at AR in bicalutamide-resistant human LNCAP cells assessed as effect on cell proliferation after 6 days
    Antagonist activity at AR in bicalutamide-resistant human LNCAP cells assessed as effect on cell proliferation after 6 days
    [PMID: 20381361]
    LNCaP IC50
    600 nM
    Compound: 3
    Antagonist activity at AR in human bicalutamide-resistant LNCAP cells assessed as inhibition of cell proliferation after 6 days
    Antagonist activity at AR in human bicalutamide-resistant LNCAP cells assessed as inhibition of cell proliferation after 6 days
    [PMID: 21050768]
    LNCaP IC50
    732.7 nM
    Compound: 2
    Antiproliferative activity against human LNCAP cells after 3 days
    Antiproliferative activity against human LNCAP cells after 3 days
    [PMID: 26046313]
    LNCaP IC50
    74 μM
    Compound: (R,S)Bicalutamide
    Cytotoxicity against androgen-dependent human LNCAP cells after 72 hrs by SRB assay
    Cytotoxicity against androgen-dependent human LNCAP cells after 72 hrs by SRB assay
    [PMID: 22672984]
    MDA-MB-435 IC50
    173 nM
    Compound: 5
    Antagonist activity at human wild type AR expressed in human MDA-MB-435 cells by transactivation assay
    Antagonist activity at human wild type AR expressed in human MDA-MB-435 cells by transactivation assay
    [PMID: 20584610]
    PC-3 IC50
    > 10 μM
    Compound: 4
    Cytotoxicity against human PC3 cells assessed as growth inhibition after 3 days by WST-8 assay
    Cytotoxicity against human PC3 cells assessed as growth inhibition after 3 days by WST-8 assay
    [PMID: 24900588]
    PC-3 IC50
    60.69 μM
    Compound: BIC
    Antiproliferative activity against AR negative human PC3 cells after 48 hrs by MTT assay
    Antiproliferative activity against AR negative human PC3 cells after 48 hrs by MTT assay
    [PMID: 28162857]
    PC-3 IC50
    76.4 μM
    Compound: (R,S)Bicalutamide
    Cytotoxicity against androgen-independent human PC3 cells after 72 hrs by SRB assay
    Cytotoxicity against androgen-independent human PC3 cells after 72 hrs by SRB assay
    [PMID: 22672984]
    PC-3 IC50
    77 μM
    Compound: Casodex
    Cytotoxicity against human androgen-independent PC3 cells by MTT assay
    Cytotoxicity against human androgen-independent PC3 cells by MTT assay
    [PMID: 22326399]
    PC-3 GI50
    9.15 μM
    Compound: Casodex
    Growth inhibition of human PC3 cells by MTT assay
    Growth inhibition of human PC3 cells by MTT assay
    [PMID: 25634130]
    SC-3 IC50
    0.67 μM
    Compound: 1
    Antiandrogen activity against androgen receptor in androgen-dependent mouse SC3 cells assessed as inhibition of testosterone-induced cell proliferation by WST1 assay
    Antiandrogen activity against androgen receptor in androgen-dependent mouse SC3 cells assessed as inhibition of testosterone-induced cell proliferation by WST1 assay
    [PMID: 20888766]
    SC-3 IC50
    3 μM
    Compound: Bicalutamide
    Antagonist activity at androgen receptor in androgen-dependent mouse SC3 cells assessed as inhibition of testosterone-induced cell growth after 3 days
    Antagonist activity at androgen receptor in androgen-dependent mouse SC3 cells assessed as inhibition of testosterone-induced cell growth after 3 days
    [PMID: 23462715]
    VCaP IC50
    64.712 μM
    Compound: 3; Casodex; Bicalutamide
    Antiproliferative activity against human VCaP cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay
    Antiproliferative activity against human VCaP cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay
    [PMID: 27131065]
    VCaP IC50
    68.37 μM
    Compound: RS-Bicalutamide
    Antiproliferative activity against human VCaP cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay
    Antiproliferative activity against human VCaP cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay
    [PMID: 27301368]
    VCaP IC50
    68.37 μM
    Compound: 3; Casodex; Bicalutamide
    Antiproliferative activity against human VCaP cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay
    Antiproliferative activity against human VCaP cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay
    [PMID: 27131065]
    VCaP IC50
    68.4 μM
    Compound: 1
    Antiproliferative activity against human VCaP cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay
    Antiproliferative activity against human VCaP cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay
    [PMID: 31288149]
    體外研究
    (In Vitro)

    在全細(xì)胞結(jié)合試驗(yàn) (LNCaP/AR (cs) 細(xì)胞) 中,Bicalutamide 與雄激素競爭結(jié)合 AR,IC50 為 160 nM[1]。
    Bicalutamide 以劑量依賴性方式誘導(dǎo) VCaP 細(xì)胞增殖,同時(shí)部分拮抗 R1881 (合成雄激素)[1]的作用。

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

    體內(nèi)研究
    (In Vivo)

    Bicalutamide (10 mg/kg;ig;每天;持續(xù) 28 天) 在前列腺癌小鼠模型中表現(xiàn)出抗腫瘤活性[1]。

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

    Animal Model: Castrate male mice, bearing LNCaP/AR(cs) xenograft tumors[1]
    Dosage: 10 mg/kg
    Administration: Oral gavage, daily, for 28 days
    Result: Inhibited tumors growth.
    Clinical Trial
    分子量

    430.37

    Formula

    C18H14F4N2O4S

    CAS 號
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    比卡魯胺

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn): 

    DMSO 中的溶解度 : ≥ 50 mg/mL (116.18 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.3236 mL 11.6179 mL 23.2358 mL
    5 mM 0.4647 mL 2.3236 mL 4.6472 mL
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲存時(shí),請?jiān)?年內(nèi)使用, -20°C儲存時(shí),請?jiān)?個(gè)月內(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?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,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;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.81 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.81 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

      2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
    動(dòng)物溶解方案計(jì)算器
    請輸入動(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

    由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
    請輸入您的動(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 2%。
    方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購。 Tween 80,均可在 MCE 網(wǎng)站選購。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
    您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(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)給藥周期超過半月以上,請謹(jǐn)慎選擇該方案。
    請確保第一步儲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: 99.85%

    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲存時(shí),請?jiān)?年內(nèi)使用, -20°C儲存時(shí),請?jiān)?個(gè)月內(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 2.3236 mL 11.6179 mL 23.2358 mL 58.0896 mL
    5 mM 0.4647 mL 2.3236 mL 4.6472 mL 11.6179 mL
    10 mM 0.2324 mL 1.1618 mL 2.3236 mL 5.8090 mL
    15 mM 0.1549 mL 0.7745 mL 1.5491 mL 3.8726 mL
    20 mM 0.1162 mL 0.5809 mL 1.1618 mL 2.9045 mL
    25 mM 0.0929 mL 0.4647 mL 0.9294 mL 2.3236 mL
    30 mM 0.0775 mL 0.3873 mL 0.7745 mL 1.9363 mL
    40 mM 0.0581 mL 0.2904 mL 0.5809 mL 1.4522 mL
    50 mM 0.0465 mL 0.2324 mL 0.4647 mL 1.1618 mL
    60 mM 0.0387 mL 0.1936 mL 0.3873 mL 0.9682 mL
    80 mM 0.0290 mL 0.1452 mL 0.2904 mL 0.7261 mL
    100 mM 0.0232 mL 0.1162 mL 0.2324 mL 0.5809 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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