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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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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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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Pexidartinib (PLX3397)

Catalog No. A15520
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CSF1/Kit/FLT3 抑制剂

Pexidartinib (PLX3397)是KIT，CSF1R和FLT3的小分子酪氨酸激酶（RTK）抑制剂，具有潜在的抗肿瘤活性。了解更多

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- Lu Luo, .et al. Intermittent theta-burst stimulation improves motor function by inhibiting neuronal pyroptosis and regulating microglial polarization via TLR4/NF κB/NLRP3 signaling pathway in cerebral ischemic mice, J Neuroinflammation, 2022, Jun 11;19(1):141 PMID: 35690810
- Sarah R Anderson,, .et al. Neuronal apoptosis drives remodeling states of microglia and shifts in survival pathway dependence, bioRxiv, 2022, 01.05.475126
- Hannah D Mason, .et al. Glia limitans superficialis oxidation and breakdown promotes cortical cell death after repeat head injury, JCI Insight, 2021, Oct 8;6(19):e149229 PMID: 34428178
- Chritica Lodder, .et al. CSF1R inhibition rescues tau pathology and neurodegeneration in an A/T/N model with combined AD pathologies, while preserving plaque associated microglia, Acta Neuropathol Commun, 2021, Jun 8;9(1):108 PMID: 34103079
- Anderson SR, .et al. Developmental Apoptosis Promotes a Disease-Related Gene Signature and Independence from CSF1R Signaling in Retinal Microglia, Cell Rep, 2019, May 14;27(7):2002-2013.e5 PMID: 31091440
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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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