VEGFR

Inhibitory Selectivity

Catalog No.	Inhibitor Name	VEGFR1	VEGFR2	VEGFR3	Other
A10001	Sorafenib Tosylate		**		Raf-1,B-Raf,B-Raf (V599E)
A10880	Sunitinib Malate		*		Kit,FLT3,PDGFRβ
A10996	Cabozantinib	***	****	***	c-Met,Kit,Axl
A10080	Ponatinib		****		Abl,PDGFRα,FGFR1
A10103	Axitinib	****	****	****	PDGFRβ,Kit,PDGFRα
A10998	Foretinib	***	****	****	Met,Tie-2,RON
A10963	Vandetanib		**	*
A10137	Nintedanib	**	***	***	LCK,FLT3,FGFR2
A10250	Regorafenib	***	****	*	RET,Raf-1,Kit
A11518	Pazopanib HCl	***	**	*	FGFR,PDGFR,c-Kit
A10185	Cediranib	***	****	****	c-Kit,PDGFRβ,FGFR1
A10703	PD173074		*		FGFR1,c-Src
A11411	Dovitinib	***	***	***	FLT3,c-Kit,FGFR1
A10025	Linifanib	****	****	*	CSF-1R,FLT3,Kit
A10967	Vatalanib 2HCl	*	**	*	PDGFRβ,c-Kit,c-Fms
A10773	RAF265		**		B-Raf
A10101	Tivozanib	**	***	**	EphB2,PDGFRα,PDGFRβ
A10608	Motesanib Diphosphate	****	****	***	Kit,RET,PDGFR
A10340	Lenvatinib	**	****	***	PDGFRβ,FGFR1,PDGFRα
A10953	Orantinib		*		PDGFRβ,FGFR1
A10254	Brivanib	*	**		FGFR1
A10587	MGCD-265	****	****	****	Met,RON,Tie-2
A10043	AEE788	*	*	*	EGFR,HER2/ErbB2,c-Abl
A10352	ENMD-2076		*	**	FLT3,RET,Aurora A
A10679	OSI-930	***	***		CSF-1R,LCK,C-Raf
A10248	CYC116		**		Aurora A,Aurora B,FLT3
A10502	Ki8751		****		c-Kit,PDGFRα,FGFR2
A10903	Telatinib		***	****	c-Kit,PDGFRα
A11518	Pazopanib	***	**	*	FGFR,PDGFR,c-Kit
A10504	KRN 633	*	*	*	PDGFRα,c-Kit,BTK
A13377	SAR131675			**
A10198	Dovitinib Dilactic Acid	***	***	***	FLT3,c-Kit,FGFR1
A11407	Apatinib		****		RET,c-Kit,c-Src
A10154	BMS-794833		**		Met
A10162	Brivanib Alaninate	*	**		FGFR1
A11396	Golvatinib		**		c-Met
A11954	ZM 323881 HCl		****
A11955	ZM 306416	*			Src,Abl
A16342	BFH772		****
A11558	SU5402		**		FGFR1,PDGFRβ
A12437	Semaxanib		*
A11244	LY2874455		***		FGFR2,FGFR1,FGFR4
A13234	SKLB1002		**
A14156	AZD2932		***		PDGFRβ,Flt3,c-Kit
A10893	Taxifolin (Dihydroquercetin)
A11772	CP-547632		***		FGFR
A12693	BAW2881 (NVP-BAW2881)	*	***	*	C-Raf-1,B-RAFV599E,c-Abl
A13465	SKLB610		*		PDGFR, FGFR2
A13819	TG 100801	****	***		FGFR1, Fyn, Src
A13820	TG 100572	****	***		FGFR1, Fyn, Src
A14387	ltiratinib (DCC2701)		***		MET, TIE2, TRK
A15073	E-3810	***	**	***	FGFR-1, FGFR-2
A15287	ZM323881		****
A15792	BMS-817378		***		c-Met

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

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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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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

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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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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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Ki8751

Catalog No. A10502
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VEGFR-2 抑制剂

ki8751是一种细胞可渗透的喹啉氧基苯基脲化合物，在基于细胞和无细胞的检测中起Flk-1 (VEGFR-2)选择性抑制剂的作用。了解更多

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- Kohei Ashina, .et al. VEGF-induced blood flow increase causes vascular hyper-permeability in vivo, Biochem Biophys Res Commun, 2015, Aug 21;464(2):590-5 PMID: 26163262
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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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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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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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