Axitinib (Synonyms: 阿昔替尼; AG-013736)

目錄號: HY-10065 純度: 99.90%: FAQs
Data Sheet SDS COA 產品使用指南

摩爾計算器

Axitinib是多靶點的酪氨酸激酶抑制劑，抑制 VEGFR1，VEGFR2，VEGFR3， PDGFRβ 的 IC₅₀ 值分別為 0.1, 0.2, 0.1-0.3, 1.6 nM。

MCE 的所有產品僅用作科學研究或藥證申報，我們不為任何個人用途提供產品和服務

Axitinib Chemical Structure

CAS No. : 319460-85-0

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規(guī)格	價格	是否有貨
10 mM * 1 mL in DMSO	￥616	In-stock
50 mg	￥560	In-stock
100 mg	￥900	In-stock
200 mg	￥1475	In-stock
500 mg	￥2613	In-stock
1 g		詢價
5 g		詢價

or 大包裝詢價

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Customer Review

Other Forms of Axitinib:

MCE 顧客使用本產品發(fā)表的 26 篇科研文獻

•Cell Metab. 2021 Sep 8;S1550-4131(21)00375-2. [Abstract]
•Cell Stem Cell. 2019 Sep 5;25(3):373-387.e9. [Abstract]
•Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. [Abstract]
•Adv Sci (Weinh). 2023 Apr 23;e2205915. [Abstract]
•Adv Healthc Mater. 2024 Oct 14:e2401985. [Abstract]
•Int J Biol Macromol. 2024 Feb 5;262(Pt 1):129950. [Abstract]

•Sci Total Environ. 2023 Aug 23;903:166505. [Abstract]
•Acta Pharmacol Sin. 2021 Jan;42(1):108-114. [Abstract]
•Cell Rep. 2016 May 10;15(6):1144-60. [Abstract]
•J Transl Med. 2023 Sep 11;21(1):614. [Abstract]
•BMC Biol. 2024 Oct 1;22(1):222. [Abstract]
•Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
•Mol Carcinog. 2024 Aug 13. [Abstract]
•Int Immunopharmacol. 2024 Apr 30:133:112145. [Abstract]
•Cancers (Basel). 2023 Nov 12, 15(22), 5375.
•Int J Mol Sci. 2022 Sep 14;23(18):10677.
•Front Immunol. 30 April 2021.
•Ther Adv Med Oncol. 2019 May 17;11:1758835919849757. [Abstract]
•Sci Pharm. 2023 Feb;91(1), 12.
•PLoS One. 2021 Nov 3;16(11):e0259241. [Abstract]
•Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
•J Cell Biochem. 2020 Mar;121(3):2343-2353. [Abstract]
•bioRxiv. 2024 Jul 1:2024.06.27.601041. [Abstract]
•Research Square Preprint. 2022 Feb.
•Patent. US20170349880A1.
•Harvard Medical School LINCS LIBRARY

Cell Viability Assay

: Axitinib purchased from MCE. Usage Cited in: Sci Pharm. 2023 Feb;91(1), 12.; Axitinib (1, 10, 30 μM; 24 h) inhibits viability of MCF-7 cells.

Axitinib 相關產品

•相關化合物庫:

•同靶點產品:

•同靶點蛋白產品:

查看 VEGFR 亞型特異性產品:

查看所有亞型

VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

查看 PDGFR 亞型特異性產品:

查看所有亞型

PDGFR PDGFRβ PDGFRα

生物活性
實驗參考方法
純度 & 產品資料
參考文獻

生物活性

Axitinib is a multi-targeted tyrosine kinase inhibitor with IC₅₀s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively.

IC₅₀ & Target^[1]

VEGFR1

0.1 nM (IC₅₀)

VEGFR2

0.2 nM (IC₅₀)

VEGFR3

0.1 nM (IC₅₀)

PDGFRβ

1.6 nM (IC₅₀)

細胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
518A2	IC₅₀	4.4 μM Compound: Axitinib	Cytotoxicity against human 518A2 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against human 518A2 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 31958738]
A549	IC₅₀	> 25 μM Compound: Axitinib	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	22.4 μM Compound: Axitinib	Antiproliferative activity against VEGF-stimulated human A549 cells after 48 hrs by CCK8 assay Antiproliferative activity against VEGF-stimulated human A549 cells after 48 hrs by CCK8 assay	[PMID: 30108994]
A549	IC₅₀	4.88 μM Compound: II	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31445229]
BaF3	GI₅₀	0.002 μM Compound: 6	Inhibition of TEL fused c-KIT V559G mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT V559G mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.005 μM Compound: 6	Inhibition of TEL fused c-KIT V559A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT V559A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.007 μM Compound: 6	Inhibition of TEL fused c-KIT L576P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT L576P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.012 μM Compound: 6	Inhibition of TEL fused c-KIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.013 μM Compound: 6	Inhibition of TEL fused c-KIT V654A/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT V654A/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.014 μM Compound: 6	Inhibition of TEL fused c-KIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.105 μM Compound: 6	Inhibition of wild type TEL fused c-KIT (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type TEL fused c-KIT (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.108 μM Compound: 6	Inhibition of TEL fused c-KIT T670I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT T670I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.11 μM Compound: 8	Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.12 μM Compound: 8	Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.129 μM Compound: 6	Inhibition of TEL fused c-KIT T670I/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT T670I/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.156 μM Compound: 6	Inhibition of TEL fused c-KIT D820E mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT D820E mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.2 μM Compound: 8	Inhibition of BCR/ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.24 μM Compound: 8	Inhibition of BCR/ABL V299L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL V299L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.35 μM Compound: 8	Inhibition of wild type BCR/ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of wild type BCR/ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.406 μM Compound: 6	Inhibition of TEL fused c-KIT A829P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT A829P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	0.83 μM Compound: 8	Inhibition of BCR/ABL Q252H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL Q252H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	0.84 μM Compound: 8	Inhibition of BCR/ABL M351T mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL M351T mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	1.01 μM Compound: 8	Inhibition of BCR/ABL H369P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL H369P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	1.46 μM Compound: 8	Inhibition of BCR/ABL F317L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL F317L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	1.64 μM Compound: 6	Antiproliferative activity in mouse BAF3 cells after 72 hrs by CCK8 assay Antiproliferative activity in mouse BAF3 cells after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	1.64 μM Compound: 8	Antiproliferative activity in mouse BAF3 cells after 72 hrs by CCK8 assay Antiproliferative activity in mouse BAF3 cells after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	1.72 μM Compound: 6	Inhibition of TEL fused c-KIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	1.82 μM Compound: 6	Inhibition of TEL fused c-KIT D816H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT D816H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	1.91 μM Compound: 8	Inhibition of BCR/ABL Y253F mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL Y253F mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
BaF3	GI₅₀	2.02 μM Compound: 6	Inhibition of TEL fused c-KIT D816V mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of TEL fused c-KIT D816V mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 31046271]
BaF3	GI₅₀	2.63 μM Compound: 8	Inhibition of BCR/ABL F317I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL F317I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay	[PMID: 30317026]
CHO	GI₅₀	> 10 μM Compound: 8	Antiproliferative activity in CHO cells after 72 hrs by CCK8 assay Antiproliferative activity in CHO cells after 72 hrs by CCK8 assay	[PMID: 30317026]
EA.hy 926	IC₅₀	6.1 μM Compound: Axitinib	Cytotoxicity against human EA.hy 926 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against human EA.hy 926 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 31958738]
HCC1954	GI₅₀	2.7 μM Compound: 1	Antiproliferative activity against human HCC1954 cells assessed as growth inhibition after 5 days by SRB assay Antiproliferative activity against human HCC1954 cells assessed as growth inhibition after 5 days by SRB assay	[PMID: 23829549]
HCT-116	IC₅₀	> 25 μM Compound: Axitinib	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	IC₅₀	> 25 μM Compound: Axitinib	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	IC₅₀	1.5 μM Compound: Axitinib	Cytotoxicity against wild type human HCT-116 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against wild type human HCT-116 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 31958738]
HCT-116	IC₅₀	1.6 μM Compound: Axitinib	Cytotoxicity against human HCT-116 p53 mutant cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against human HCT-116 p53 mutant cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 31958738]
HEK-293T	IC₅₀	46.82 μM Compound: II	Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31445229]
HepG2	IC₅₀	38.7 μM Compound: Axitinib	Antiproliferative activity against VEGF-stimulated human HepG2 cells after 48 hrs by CCK8 assay Antiproliferative activity against VEGF-stimulated human HepG2 cells after 48 hrs by CCK8 assay	[PMID: 30108994]
HL-60	GI₅₀	6.78 μM Compound: 8	Antiproliferative activity in human HL60 cells after 72 hrs by CCK8 assay Antiproliferative activity in human HL60 cells after 72 hrs by CCK8 assay	[PMID: 30317026]
HT-29	IC₅₀	13.12 μM Compound: II	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31445229]
K562	GI₅₀	0.94 μM Compound: 8	Antiproliferative activity in human K562 cells after 72 hrs by CCK8 assay Antiproliferative activity in human K562 cells after 72 hrs by CCK8 assay	[PMID: 30317026]
KB-V1	IC₅₀	12.9 μM Compound: Axitinib	Cytotoxicity against multidrug resistant human KB-V1 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against multidrug resistant human KB-V1 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 31958738]
KU812 cell line	GI₅₀	0.5 μM Compound: 8	Antiproliferative activity in human KU812 cells after 72 hrs by CCK8 assay Antiproliferative activity in human KU812 cells after 72 hrs by CCK8 assay	[PMID: 30317026]
MCF7	IC₅₀	> 25 μM Compound: Axitinib	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	GI₅₀	0.97 μM Compound: 1	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 5 days by SRB assay Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 5 days by SRB assay	[PMID: 23829549]
MCF7	GI₅₀	2.3 μM Compound: 3	Cytotoxicity against human MCF7 cells after 5 days by SRB assay Cytotoxicity against human MCF7 cells after 5 days by SRB assay	[PMID: 24867403]
MDA-MB-231	GI₅₀	11 μM Compound: 3	Cytotoxicity against human MDA-MB-231 cells after 5 days by SRB assay Cytotoxicity against human MDA-MB-231 cells after 5 days by SRB assay	[PMID: 24867403]
MDA-MB-231	GI₅₀	7.3 μM Compound: 1	Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 5 days by SRB assay Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 5 days by SRB assay	[PMID: 23829549]
MDA-MB-468	GI₅₀	1.3 μM Compound: 1	Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition after 5 days by SRB assay Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition after 5 days by SRB assay	[PMID: 23829549]
MDA-MB-468	GI₅₀	2.8 μM Compound: 3	Cytotoxicity against human MDA-MB-468 cells after 5 days by SRB assay Cytotoxicity against human MDA-MB-468 cells after 5 days by SRB assay	[PMID: 24867403]
MEC1	GI₅₀	1.54 μM Compound: 8	Antiproliferative activity in human MEC1 cells after 72 hrs by CCK8 assay Antiproliferative activity in human MEC1 cells after 72 hrs by CCK8 assay	[PMID: 30317026]
MEG-01	GI₅₀	0.97 μM Compound: 8	Antiproliferative activity in human MEG01 cells after 72 hrs by CCK8 assay Antiproliferative activity in human MEG01 cells after 72 hrs by CCK8 assay	[PMID: 30317026]
NHDF	IC₅₀	> 25 μM Compound: Axitinib	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]
OCI-AML2	GI₅₀	2.36 μM Compound: 8	Antiproliferative activity in human OCI-AML2 cells after 72 hrs by CCK8 assay Antiproliferative activity in human OCI-AML2 cells after 72 hrs by CCK8 assay	[PMID: 30317026]
PC-3	IC₅₀	16.43 μM Compound: II	Cytotoxicity against human PC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31445229]
Sf9	IC₅₀	0.0002 μM Compound: 8	Inhibition of active wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay Inhibition of active wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay	[PMID: 30317026]
Sf9	IC₅₀	0.001 μM Compound: 8	Inhibition of inactive wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8 Inhibition of inactive wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8	[PMID: 30317026]
Sf9	IC₅₀	0.092 μM Compound: 8	Inhibition of inactive wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8 hrs by ADP-G Inhibition of inactive wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8 hrs by ADP-G	[PMID: 30317026]
Sf9	IC₅₀	0.17 μM Compound: 8	Inhibition of active wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay Inhibition of active wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay	[PMID: 30317026]
Sf9	IC₅₀	39 nM Compound: II	Inhibition of recombinant human N-terminal GST-tagged VEGFR2 (805 to 1356 residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate incubated for 45 mins by kinase-Glo luminescent assay Inhibition of recombinant human N-terminal GST-tagged VEGFR2 (805 to 1356 residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate incubated for 45 mins by kinase-Glo luminescent assay	[PMID: 31445229]
SK-BR-3	GI₅₀	3.8 μM Compound: 1	Antiproliferative activity against human SKBR3 cells assessed as growth inhibition after 5 days by SRB assay Antiproliferative activity against human SKBR3 cells assessed as growth inhibition after 5 days by SRB assay	[PMID: 23829549]
SK-BR-3	GI₅₀	4.6 μM Compound: 3	Cytotoxicity against human SKBR3 cells after 5 days by SRB assay Cytotoxicity against human SKBR3 cells after 5 days by SRB assay	[PMID: 24867403]
U-87MG ATCC	IC₅₀	21.7 μM Compound: II	Cytotoxicity against human U87MG cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human U87MG cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31445229]
U-937	GI₅₀	1.98 μM Compound: 8	Antiproliferative activity in human U937 cells after 72 hrs by CCK8 assay Antiproliferative activity in human U937 cells after 72 hrs by CCK8 assay	[PMID: 30317026]

體外研究
(In Vitro)

Axitinib (AG-013736) 是一種有效的選擇性 VEGFR 1 至 3 抑制劑。在轉染或內源性 RTK 表達細胞中，Axitinib 有效阻斷生長因子刺激的 VEGFR-2 和 VEGFR-3 磷酸化，平均 IC₅₀ 值分別為 0.2 和 0.1 至 0.3 nM?；?Axitinib 的蛋白結合，針對 VEGFR-1 的細胞活性為 1.2 nM (在存在 2.3% 牛血清白蛋白的情況下測量)，相當于絕對 IC₅₀ ~0.1 nM。在 Flk-1 轉染的 NIH-3T3 細胞中針對鼠 VEGFR-2 (Flk-1) 的效力為 0.18 nM，與其人類同系物相似。Axitinib 對密切相關的 III 型和 V 型家族 RTK，包括 PDGFR-β (1.6 nM)、KIT (1.7 nM) 和 PDGFR-α，顯示出約 8 至 25 倍的 IC₅₀ (5 nM)；納摩爾濃度的 Axitinib 可阻斷 PDGF BB 介導的人神經(jīng)膠質瘤 U87MG 細胞 (PDGFR-β 陽性) 遷移，但不會阻斷增殖^[2]。

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

體內研究
(In Vivo)

與對照腫瘤相比，單次口服劑量的 Axitinib (100 mg/kg) 顯著抑制小鼠 VEGFR-2 磷酸化長達 7 小時。Axitinib 快速抑制 VEGF 誘導的小鼠皮膚血管通透性；這種抑制是劑量依賴性的，并且與小鼠體內的藥物濃度直接相關。藥代動力學/藥效學分析表明未結合的 EC₅₀ 為 0.46 nM。在沒有外源性 VEGF-A 刺激的 MV522 荷瘤小鼠的皮膚中也顯示出類似的抑制作用。Axitinib 抑制小鼠人異種移植腫瘤的生長。無論初始腫瘤大小、模型類型或植入部位如何，阿西替尼都會產生劑量依賴性生長延遲^[2]。

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

Clinical Trial

分子量

386.47

Formula

C₂₂H₁₈N₄OS

CAS 號

319460-85-0

性狀

固體

顏色

White to light yellow

中文名稱

阿昔替尼；阿西替尼

運輸條件

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	2 years
	-20°C	1 year

溶解性數(shù)據(jù)

細胞實驗：

DMSO 中的溶解度 : 20.83 mg/mL (53.90 mM; 超聲助溶; 吸濕的 DMSO 對產品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液

濃度溶劑體積質量	1 mg	5 mg	10 mg

1 mM	2.5875 mL	12.9376 mL	25.8752 mL
5 mM	0.5175 mL	2.5875 mL	5.1750 mL
10 mM	0.2588 mL	1.2938 mL	2.5875 mL

查看完整儲備液配制表

* 請根據(jù)產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，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內使用， -20°C儲存時，請在1年內使用。

摩爾計算器
稀釋計算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動物實驗：

請根據(jù)您的實驗動物和給藥方式選擇適當?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：
——為保證實驗結果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
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: ≥ 2.08 mg/mL (5.38 mM); 澄清溶液

此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 20.8 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: 2.08 mg/mL (5.38 mM); 懸濁液; 超聲助溶

此方案可獲得 2.08 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。
以 1 mL 工作液為例，取 100 μL 20.8 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。
方案三

請依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.38 mM); 澄清溶液

此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液，此方案實驗周期在半個月以上的動物實驗酌情使用。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內盡快用完。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： 20% HP-β-CD/10 mM Citrate pH 2.0
Solubility: 8.33 mg/mL (21.55 mM); 澄清溶液; Need ultrasonic and adjust pH to 3 with H₂O

動物溶解方案計算器

請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

每只動物的給藥體積

μL

動物數(shù)量

只

由于實驗過程有損耗，建議您多配一只動物的量

請輸入您的動物體內配方組成：

DMSO +

Tween-80 +

Saline

如果您的動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。

計算結果

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品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術支持聯(lián)系。

動物實驗體內工作液的配制方法 : 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 & 產品資料

純度: 99.94%

選擇批次：

Data Sheet (661 KB) SDS (597 KB)

COA (291 KB) HNMR (256 KB) LCMS (187 KB) 元素分析報告 (214 KB)

產品使用指南 (1538 KB)

參考文獻

[1]. Fenton BM, et al. The addition of AG-013736 to rractionated radiation improves tumor response without functionally normalizing the tumor vasculature. Cancer Res. 2007 Oct 15;67(20):9921-8. [Content Brief]

[2]. Hu-Lowe DD, et al. Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2, 3. Clin Cancer Res. 2008 Nov 15;14(22):7272-83 [Content Brief]

[3]. Allen E, et al. Metabolic Symbiosis Enables Adaptive Resistance to Anti-angiogenic Therapy that Is Dependent on mTOR Signaling. Cell Rep. 2016 May 10;15(6):1144-60. [Content Brief]

Cell Assay ^[2]	Endothelial or tumor cells are starved for 18 h in the presence of either 1% FBS (HUVEC) or 0.1% FBS (tumor cells). Axitinib is added and cells are incubated for 45 min at 37°C in the presence of 1 mM Na₃VO₄. The appropriate growth factor is added to the cells, and after 5 min, cells are rinsed with cold PBS and lysed in the lysis buffer and a protease inhibitor cocktail. The lysates are incubated with immunoprecipitation antibodies for the intended proteins overnight at 4°C. Antibody complexes are conjugated to protein A beads and supernatants are separated by SDS-PAGE^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice and Rats^[2] Mice with M24met xenograft tumors (400-600 mm³) are administered with a single dose of Axitinib or the control (0.5% carboxymethylcellulose/H₂O). Blood and tumor tissue samples are collected for pharmacokinetic and VEGFR-2 measurements. Total protein concentrations in tumor tissues are determined using the Bradford colorimetric assay. Six-day-old Sprague-Dawley rats are given two i.p. injections of Axitinib (30 mg/kg ). Animals are sacrificed, retinas are collected and lysed, and immunoprecipitation/immunoblotting experiments are done. ECL-Plus is used for detection and densitometry analysis is done using the Alpha Imager 8800. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻	[1]. Fenton BM, et al. The addition of AG-013736 to rractionated radiation improves tumor response without functionally normalizing the tumor vasculature. Cancer Res. 2007 Oct 15;67(20):9921-8. [Content Brief] [2]. Hu-Lowe DD, et al. Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2, 3. Clin Cancer Res. 2008 Nov 15;14(22):7272-83 [Content Brief] [3]. Allen E, et al. Metabolic Symbiosis Enables Adaptive Resistance to Anti-angiogenic Therapy that Is Dependent on mTOR Signaling. Cell Rep. 2016 May 10;15(6):1144-60. [Content Brief]

Axitinib 相關分類

完整儲備液配制表

可選溶劑	濃度溶劑體積質量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5875 mL	12.9376 mL	25.8752 mL	64.6881 mL
	5 mM	0.5175 mL	2.5875 mL	5.1750 mL	12.9376 mL
	10 mM	0.2588 mL	1.2938 mL	2.5875 mL	6.4688 mL
	15 mM	0.1725 mL	0.8625 mL	1.7250 mL	4.3125 mL
	20 mM	0.1294 mL	0.6469 mL	1.2938 mL	3.2344 mL
	25 mM	0.1035 mL	0.5175 mL	1.0350 mL	2.5875 mL
	30 mM	0.0863 mL	0.4313 mL	0.8625 mL	2.1563 mL
	40 mM	0.0647 mL	0.3234 mL	0.6469 mL	1.6172 mL
	50 mM	0.0518 mL	0.2588 mL	0.5175 mL	1.2938 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.

Keywords:

Axitinib319460-85-0AG-013736阿昔替尼阿西替尼AG013736AG 013736VEGFRPDGFRVascular endothelial growth factor receptorPlatelet-derived growth factor receptorInhibitorinhibitorinhibit

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Axitinib (Synonyms: 阿昔替尼; AG-013736)

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MCE 顧客使用本產品發(fā)表的 26 篇科研文獻

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生物活性

實驗參考方法

純度 & 產品資料

參考文獻

摩爾計算器

稀釋計算器

Axitinib 相關分類

完整儲備液配制表

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Axitinib (Synonyms: 阿昔替尼; AG-013736)

Customer Review

Other Forms of Axitinib:

Axitinib 相關抗體

MCE 顧客使用本產品發(fā)表的 26 篇科研文獻

Axitinib 相關產品

•相關化合物庫:

•同靶點產品:

•同靶點蛋白產品:

查看 VEGFR 亞型特異性產品:

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實驗參考方法

純度 & 產品資料

參考文獻

Axitinib 相關抗體:

摩爾計算器

稀釋計算器

Axitinib 相關分類

完整儲備液配制表

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