製品番号: HY-10065

アキシチニブ

(別名: Axitinib; AG-013736)

42 Cited Publications

カスタマーレビュー

Based on 42 publication(s) in Google Scholar

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.

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純度: 99.84%
CAS 番号: 319460-85-0
分子式: C₂₂H₁₈N₄OS
分子量:386.47

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Axitinib 構造式

CAS 番号: 319460-85-0

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生物活性
- 製品説明
- IC₅₀ & Target
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化学情報
Publications (42)
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製品説明

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)

VEGFR アイソフォーム固有の製品をすべて表示 :

PDGFR アイソフォーム固有の製品をすべて表示 :

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 H396P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay Inhibition of BCR/ABL H396P 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]
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]
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]
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]

体外実験

Axitinib (AG-013736) is a potent and selective inhibitor of VEGFR 1 to 3. In transfected or endogenous RTK-expressing cells, Axitinib potently blocks growth factor-stimulated phosphorylation of VEGFR-2 and VEGFR-3 with average IC₅₀ values of 0.2 and 0.1 to 0.3 nM, respectively. Cellular activity against VEGFR-1 is 1.2 nM (measured in the presence of 2.3% bovine serum albumin), equivalent to an absolute IC₅₀ of ~0.1 nM, based on protein binding of Axitinib. The potency against murine VEGFR-2 (Flk-1) in Flk-1-transfected NIH-3T3 cells is 0.18 nM, similar to that of its human homologue. Axitinib shows ~8- to 25-fold higher IC₅₀ against the closely related type III and V family RTKs, including PDGFR-β (1.6 nM), KIT (1.7 nM), and PDGFR-α (5 nM); nanomolar concentrations of Axitinib blocks PDGF BB-mediated human glioma U87MG cell (PDGFR-β-positive) migration but not proliferation^[2].

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

体内実験

A single oral dose of Axitinib (100 mg/kg) markedly suppresses murine VEGFR-2 phosphorylation for up to 7 h compared with control tumors. Axitinib rapidly inhibits VEGF-induced vascular permeability in the skin of mice; the inhibition is dose-dependent and directly correlated with drug concentration in mice. Pharmacokinetic/pharmacodynamic analysis indicate an unbound EC₅₀ of 0.46 nM. Similar inhibitory effects are also shown in the skin of MV522 tumor-bearing mice without exogenous VEGF-A stimulation. Axitinib inhibits the growth of human xenograft tumors in mice. Axitinib produces dose-dependent growth delay regardless of initial tumor size, model type, or implant site^[2].

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

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 319460-85-0
性状 Solid
分子量 386.47
分子式 C₂₂H₁₈N₄OS
Color White to light yellow
SMILES

O=C(C1=C(SC2=CC3=C(C(/C=C/C4=CC=CC=N4)=NN3)C=C2)C=CC=C1)NC
別名

Axitinib; AG-013736
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (42)

All In Vivo Efficacy StudyCell Proliferation/Viability AssayWBFlow Cytometry

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Journal Impact Factor

Cancer Cell

Effective targeting of PDGFRA-altered high-grade glioma with avapritinib. [Abstract]

2025 Apr 14;43(4):740-756.e8. PMID: 40086436
Cell Metab

The thermogenic activity of adjacent adipocytes fuels the progression of ccRCC and compromises anti-tumor therapeutic efficacy. [Abstract]

2021 Oct 5;33(10):2021-2039.e8. PMID: 34508696
Cell Stem Cell

Generation of Human PSC-Derived Kidney Organoids with Patterned Nephron Segments and a De Novo Vascular Network. [Abstract]

2019 Sep 5;25(3):373-387.e9. PMID: 31303547
Cell Death Differ

DR5/WDR12 balances p65 stability promoting sunitinib resistance in renal cell carcinoma. [Abstract]

2026 Mar 23. PMID: 41872532
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Adv Sci (Weinh)

BEST1 Positive Monocytes in Circulation: Visualize Intratumoral Crosstalk between Cancer Cells and Monocytes. [Abstract]

2023 Jun;10(17):e2205915. PMID: 37088729
J Nanobiotechnology

Single BMSC-derived cartilage organoids for gradient heterogeneous osteochondral regeneration by leveraging native vascular microenvironment. [Abstract]

2025 Apr 29;23(1):325. PMID: 40301867
Cell Rep Med

CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]

2025 Apr 2:102053. PMID: 40187357
Cancer Lett

Chemoresistance-motility signature of molecular evolution to chemotherapy in non-muscle-invasive bladder cancer and its clinical implications. [Abstract]

2024 Nov 26:217339. PMID: 39608442
Cell Death Dis

STX17-DT facilitates axitinib resistance in renal cell carcinoma by inhibiting mitochondrial ROS accumulation and ferroptosis. [Abstract]

2025 Feb 23;16(1):125. PMID: 39988631
Adv Healthc Mater

Macrophage Membrane-Biomimetic Multi-Layered Nanoparticles Targeting Synovial Angiogenesis for Osteoarthritis Therapy. [Abstract]

2025 Jan;14(2):e2401985. PMID: 39402771
Int J Biol Macromol

Downregulation of VEGFA accelerates AGEs-mediated nucleus pulposus degeneration through inhibiting protective mitophagy in high glucose environments. [Abstract]

2024 Feb 5;262(Pt 1):129950. PMID: 38320636
Acta Pharmacol Sin

VEGFD/VEGFR3 signaling contributes to the dysfunction of the astrocyte IL-3/microglia IL-3Rα cross-talk and drives neuroinflammation in mouse ischemic stroke. [Abstract]

2025 Feb;46(2):292-307. PMID: 39478160
Acta Pharmacol Sin

Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]

2021 Jan;42(1):108-114. PMID: 32398685
Phytomedicine

Membrane cholesterol-dependent dual VEGFR2/FGFR1 inhibition by ginsenoside Rg3 to overcome gefitinib resistance in NSCLC. [Abstract]

2025 Nov 25:148:157421. PMID: 41192258
Sci Total Environ

Azithromycin induces neurotoxicity in zebrafish by interfering with the VEGF/Notch signaling pathway. [Abstract]

2023 Dec 10:903:166505. PMID: 37625730
J Transl Med

Tamoxifen exerts anti-peritoneal fibrosis effects by inhibiting H19-activated VEGFA transcription. [Abstract]

2023 Sep 11;21(1):614. PMID: 37697303
Cell Death Discov

CXCR4, CXCR7 and PBRM1 are responsible for everolimus and cabozantinib resistance in human renal cancer cells. [Abstract]

2026 Mar 28. PMID: 41896541
Cell Rep

Metabolic Symbiosis Enables Adaptive Resistance to Anti-angiogenic Therapy that Is Dependent on mTOR Signaling. [Abstract]

2016 May 10;15(6):1144-60. PMID: 27134166
Oncoimmunology

Sequential axitinib and survivin vaccination unlock curative PD-1 immunotherapy in renal carcinoma. [Abstract]

2026 Dec 31;15(1):2689769. PMID: 42343214
Front Immunol

Anti-Angiogenic Efficacy of PSORI-CM02 and the Associated Mechanism in Psoriasis In Vitro and In Vivo. [Abstract]

2021 Apr 30:12:649591. PMID: 33995368
Biol Direct

GAMT facilitates tumor progression via inhibiting p53 in clear cell renal cell carcinoma. [Abstract]

2025 Apr 2;20(1):43. PMID: 40176130
Int J Mol Sci

Chidamide plus Tyrosine Kinase Inhibitor Remodel the Tumor Immune Microenvironment and Reduce Tumor Progression When Combined with Immune Checkpoint Inhibitor in Naïve and Anti-PD-1 Resistant CT26-Bearing Mice. [Abstract]

2022 Sep 14;23(18):10677. PMID: 36142591
Bioorg Chem

Inhibition of FLT3-induced signalling in refractory acute myeloid leukaemia. [Abstract]

2025 Apr 5:160:108424. PMID: 40209351
Int Immunopharmacol

Comprehensive quantifications of tumour microenvironment to predict the responsiveness to immunotherapy and prognosis for paediatric neuroblastomas. [Abstract]

2024 May 30:133:112145. PMID: 38691920
BMC Biol

VEGF-dependent testicular vascularisation involves MEK1/2 signalling and the essential angiogenesis factors, SOX7 and SOX17. [Abstract]

2024 Oct 1;22(1):222. PMID: 39354506
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
Cancers (Basel)

Antitumor Activity of Axitinib in Lung Carcinoids: A Preclinical Study. [Abstract]

2023 Nov 12;15(22):5375. PMID: 38001635
Ther Adv Med Oncol

Axitinib overcomes multiple imatinib resistant cKIT mutations including the gatekeeper mutation T670I in gastrointestinal stromal tumors. [Abstract]

2019 May 17:11:1758835919849757. PMID: 31205508

Axitinib purchased from MedChemExpress. Usage Cited in: Ther Adv Med Oncol. 2019 May 17:11:1758835919849757. [Abstract]

Crystal violet staining of colonies from the four human GIST cell lines treated for 15 days with the indicated doses of Axitinib, imatinib, sunitinib, and regorafenib was performed.

Axitinib purchased from MedChemExpress. Usage Cited in: Ther Adv Med Oncol. 2019 May 17:11:1758835919849757. [Abstract]

The effects of Axitinib (0–3 μM; 1 h) on cellular signaling, cell cycle progression, and apoptosis in human gastrointestinal stromal tumor (GIST) cancer cell lines were examined. Immunoblotting analysis of indicated proteins in c-KIT mediated signaling pathways of GIST-T1 was performed.

Axitinib purchased from MedChemExpress. Usage Cited in: Ther Adv Med Oncol. 2019 May 17:11:1758835919849757. [Abstract]

Cell cycle analysis of the effect of Axitinib (0.3–3 μM; 24–48 h) at different concentrations in human GIST cell lines was measured by flow cytometry. Imatinib and sunitinib were used as positive controls.

Axitinib purchased from MedChemExpress. Usage Cited in: Ther Adv Med Oncol. 2019 May 17:11:1758835919849757. [Abstract]

Cell viability assessment of primary cells from three GIST patients, relative to DMSO-treated condition, after 6 days of treatment with Axitinib (0.1–3 μM) at different concentrations using the Cell Titer-Glo assay was performed.
Neurochem Res

A Novel Mutation in Exon 10 of the NOTCH3 Gene in Human Cerebral Microvascular Endothelial Cells Induces CADASIL-Like Pathology and the Therapeutic Effect of Edaravone Dexborneol on Hereditary and Non-hereditary Cerebral Small Vessel Disease. [Abstract]

2025 Nov 12;50(6):356. PMID: 41222721
Bioengineering (Basel)

Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]

2025 Oct 19;12(10):1121. PMID: 41155119
Exp Cell Res

Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]

2020 Aug 1;393(1):112054. PMID: 32376287
Mol Carcinog

Pyroptosis-related gene GSDMC indicates poor prognosis and promotes tumor progression by activating the AKT/mTOR pathway in lung squamous cell carcinoma. [Abstract]

2024 Nov;63(11):2218-2236. PMID: 39136610
J Cell Biochem

Vascular endothelial growth factor enhances tendon-bone healing by activating Yes-associated protein for angiogenesis induction and rotator cuff reconstruction in rats. [Abstract]

2020 Mar;121(3):2343-2353. PMID: 31633245
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
PLoS One

The glutaminase inhibitor telaglenastat enhances the antitumor activity of signal transduction inhibitors everolimus and cabozantinib in models of renal cell carcinoma. [Abstract]

2021 Nov 3;16(11):e0259241. PMID: 34731180

Axitinib purchased from MedChemExpress. Usage Cited in: PLoS One. 2021 Nov 3;16(11):e0259241. [Abstract]

Tumor volumes were measured in mice implanted subcutaneously with Caki-1 RCC cells and treated with either vehicle, Axitinib (25 mg/kg dosed orally QD) alone, or combinations of telaglenastat with each.
Sci Pharm

2023 Feb;91(1), 12.

Axitinib purchased from MedChemExpress. Usage Cited in: Sci Pharm. 2023 Feb;91(1), 12.

Axitinib (1, 10, 30 µM; 24 h) inhibits viability of MCF-7 cells.
Res Sq

2026 Jun 13.
bioRxiv

A TSST-1 structural motif disrupts endothelial programs required for vascular regeneration. [Abstract]

2026 May 13:2026.05.12.724633. PMID: 42182398
bioRxiv

Sulfur Amino Acid Restriction Enhances Exercise Capacity in Mice by Boosting Fat Oxidation in Muscle. [Abstract]

2024 Jul 1:2024.06.27.601041. PMID: 39005372
Research Square Preprint

2022 Feb.
Patent

US20170349880A1.

溶剤 & 溶解度

体外:

DMSO : 20.83 mg/mL (53.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (5.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.08 mg/mL (5.38 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 20% HP-β-CD/10 mM Citrate pH 2.0

Solubility: 8.33 mg/mL (21.55 mM); Clear solution; Need ultrasonic and adjust pH to 3 with H₂O

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

プロトコル

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].

MedChemExpress (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.

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (283 KB)
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- Portuguese - PT (537 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	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

Keywords

Axitinib

42 Cited Publications

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MedChemExpress（MCE）の使用を引用している文献 Axitinib

VEGFR アイソフォーム固有の製品をすべて表示

PDGFR アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (42)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Axitinib 関連分類

HY-10065 関連分類