c-Kit

Inhibitory Selectivity

Catalog No.	Inhibitor Name	c-Kit	Other
A10290	Dasatinib	***	Abl,Src
A10468	Imatinib Mesylate	**	PDGFR,v-Abl
A10996	Cabozantinib	***	VEGFR2/KDR,c-Met,VEGFR3/FLT4
A10103	Axitinib	****	VEGFR1/FLT1,VEGFR2/Flk1,VEGFR2/KDR
A10699	Pazopanib HCl	*	VEGFR1,VEGFR2,VEGFR3
A11411	Dovitinib	****	FLT3,FGFR1,VEGFR3/FLT4
A10967	Vatalanib 2HCl	*	VEGFR2/KDR,VEGFR1/FLT1,VEGFR2/Flk1
A10558	Masitinib	*	Lyn B,PDGFRα,PDGFRβ
A10101	Tivozanib	**	VEGFR2,VEGFR3,EphB2
A10610	Amuvatinib	***	PDGFRα (V561D),FLT3 (D835Y)
A10608	Motesanib Diphosphate	***	VEGFR1,VEGFR2,VEGFR2/Flk1
A10679	OSI-930	**	FLT1,KDR,CSF-1R
A10502	Ki8751	**	VEGFR2,PDGFRα,FGFR2
A10903	Telatinib	****	VEGFR3,VEGFR2,PDGFRα
A11518	Pazopanib	*	VEGFR1,VEGFR2,VEGFR3
A10198	Dovitinib Dilactic Acid	****	FLT3,FGFR1,VEGFR3/FLT4
A16320	Dasatinib Monohydrate	***	Abl ,Src
A14156	AZD2932	***	PDGFRβ,Flt3,VEGFR-2
A10880	Sunitinib Malate		FLT3,PDGFRβ,VEGFR2
A15062	DCC-2618	***	PDGFRα, PDGFRβ
A15519	PLX647	***	Fms
A15520	Pexidartinib (PLX3397)	***	CSF-1R, Flt-3

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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AC710

Catalog No. A15933
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FLT3/KIT/PDGFRα/PDGFRβ 抑制剂

AC710是一种有效的，具有活性的，选择性血小板衍生的生长因子受体家族激酶抑制剂，具有潜在的抗癌活性。了解更多

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Pazopanib (GW-786034)

Catalog No. A11518
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VEGFR 抑制剂

Pazopanib (GW-786034)是VEGFR-1，VEGFR-2，VEGFR-3，PDGFR-a/β和c-kit的有效且选择性的多靶点酪氨酸激酶抑制剂，可阻止肿瘤生长并抑制血管生成。了解更多

Product Citations (3)

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- Koide H, .et al. Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1, Xenobiotica, 2018, Oct;48(10):1059-1071 PMID: 29034773
- Ellawatty WEA, .et al. Organic cation transporter 1 is responsible for hepatocellular uptake of the tyrosine kinase inhibitor pazopanib, Drug Metab Dispos, 2018, Jan;46(1):33-40 PMID: 29089306
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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AC710 Mesylate

Catalog No. A16246
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FLT3/KIT/PDGFRα/PDGFRβ 抑制剂

AC710 Mesylate是一种有效的选择性PDGFR家族激酶抑制剂，对于FLT3/KIT/PDGFRα/PDGFRβ的Kd值分别为0.6 nM/1.0 nM/1.3 nM/1.0 nM。了解更多

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Dovitinib (TKI-258)

Catalog No. A11411
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RTK 抑制剂

Dovitinib是一种小分子多靶点酪氨酸激酶抑制剂，可抑制通过ZNF198-FGFR1或BCR-FGFR1转化为IL3独立性的Ba / F3细胞，IC50值分别为150 nM和90 nM。了解更多

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- Yunping Hu, .et al. FGFR1/MAPK-directed brachyury activation drives PD-L1-mediated immune evasion to promote lung cancer progression, Cancer Lett, 2022, Oct 28;547:215867 PMID: 35985510
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Masitinib mesylate

Catalog No. A15152
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KIT/PDGFR 抑制剂

Masitinib mesylate是Kit和PDGFRα/β的新型抑制剂，IC50为200 nM和540 nM/800 nM，对ABL和c-Fms的抑制作用较弱。了解更多

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- Julia M Harrison, .et al. Muscle fiber-type specific terminal Schwann cell pathology leads to sprouting deficits following partial denervation in SOD1 G93A mice, Neurobiol Dis, 2020, Aug 20;145:105052 PMID: 32827689
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Dovitinib Dilactic acid (TKI258 Dilactic acid)

Catalog No. A10198
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RTK 抑制剂

Dovitinib是一种小分子多靶点酪氨酸激酶抑制剂，可抑制通过ZNF198-FGFR1或BCR-FGFR1转化为IL3独立性的Ba / F3细胞，IC50值分别为150 nM和90 nM。了解更多

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N-Desethyl Sunitinib

Catalog No. A15182
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VEGFR/PDGFRβ/KIT 抑制剂

N-Desethyl Sunitinib是舒尼替尼的主要药理活性代谢产物，是有效的，ATP竞争性VEGFR，PDGFRβ和KIT抑制剂（VEGFR -1，-2，-3的Ki值为2、9、17、8和4 nM。分别为PDGFRβ和KIT）。了解更多

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Regorafenib monohydrate

Catalog No. A15218
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Tyrosine kinase 抑制剂

Regorafenib monohydrate是VEGFR1/VEGFR2/VEGFR3/PDGFRβ/Kit/RET和Raf-1的多靶点抑制剂，IC50分别为13 nM/4.2 nM/46 nM/22 nM/7 nM/1.5 nM和2.5 nM。了解更多

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