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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Regorafenib (BAY 73-4506)

Catalog No. A10250
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VEGFR 抑制剂

Regorafenib (BAY 73-4506)是一种多激酶抑制剂，IC50为17、40和69 nM c-KIT，VEGFR2，B-Raf。Regorafenib（BAY 73-4506）是一种针对肿瘤及其脉管系统的口服生物利用型多激酶抑制剂。了解更多

Product Citations (9)

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- Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. Milciclib and sorafenib synergistically downregulate c-Myc to suppress tumor growth in an orthotopic murine model of human hepatocellular carcinoma, J Transl Sci, 2020, 7: 1-10
- Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
- Mariko Fujisawa, .et al. Involvement of the Interferon Signaling Pathways in Pancreatic Cancer Cells, Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
- Sunil Kumar Yadava, .et al. Low Temperature, Easy Scaling Up Method for Development of Smart Nanostructure Hybrid Lipid Capsules for Drug Delivery Application, Colloids Surf B Biointerfaces, 2020, Mar 2;190:110927 PMID: 32169777
- Takeshi Uenaka, .et al. In silico drug screening by using genome-wide association study data repurposed dabrafenib, an anti-melanoma drug, for Parkinson's disease, Hum Mol Genet, 2018, Nov 15; 27(22): 3974-3985 PMID: 30137437
- Yi Xu, .et al. Knockdown of delta-5-desaturase promotes the anti-cancer activity of dihomo-γ-linolenic acid and enhances the efficacy of chemotherapy in colon cancer cells expressing COX-2, Free Radic Biol Med, 2016, Jul; 96: 67-77 PMID: 27101738
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AST 487

Catalog No. A15003
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RET kinase 抑制剂

AST487是Ret激酶抑制剂/FLT3抑制剂，对Ret的IC50为0.88 uM。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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