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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JI-101

Catalog No. A13545
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VEGFR2/PDGFRβ/EphB4 抑制剂

JI-101是一种具有血管内皮生长因子受体2（VEGFR2），血小板源性生长因子受体β（PDGFRβ）和ephrin B4受体B4（EphB4）的口服活性抑制剂，具有潜在的抗血管生成和抗肿瘤活性。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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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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TAK-593

Catalog No. A13555
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VEGFR/PDGFR 抑制剂

TAK-5933是一种口服制剂，其中含有血管内皮生长因子受体（VEGFR）和血小板衍生生长因子受体（PDGFR）的小分子受体酪氨酸激酶抑制剂，具有潜在的抗肿瘤活性。了解更多

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R1530

Catalog No. A13111
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Chk2, KDR, FGFR, Aurora A & Cdk2 抑制剂

R1530是吡唑并苯并二氮杂小分子，具有潜在的抗血管生成和抗肿瘤活性。R1530也是一种有丝分裂-血管生成抑制剂(MAI),可抑制多种参与血管生成的受体酪氨酸激酶，如血管内皮生长因子受体(VEGFR)-1，-2，-3，血小板衍生生长因子受体(PDGFR)βFMS样酪氨酸激酶(Flt)-3和成纤维细胞生长因子受体(FGFR) -1，-2。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

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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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SU-5402

Catalog No. A11558
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VEGFR/FGFR/EGFR 抑制剂?

SU-5402是有效且选择性的血管内皮生长因子受体(VEGFR)和成纤维细胞生长因子受体(FGFR)抑制剂(在VEGFR2, FGFR1, PDGFRβ和EGFR处IC50值分别为0.02、0.03、0.51和> 100μM)。了解更多

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- Yan Zhang, etc. Endogenously produced FGF2 is essential for the survival and proliferation of cultured mouse spermatogonial stem cells. Cell Res. 2012 Apr; 22(4): 773–776.
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Sorafenib Tosylate (Nexavar)

Catalog No. A10001
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Raf 抑制剂

Sorafenib Tosylate (Nexavar)是几种酪氨酸蛋白激酶(VEGFR和PDGFR)和RAF/MEK/ERK级联抑制剂的新型小分子抑制剂，Raf-1，wt BRAF和V599E突变型BRAF的IC50为6、22、38 nM。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
- 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
- Fangyuan Lai, .et al. Platelet-rich plasma enhances the proliferation of human adipose stem cells through multiple signaling pathways, Stem Cell Res Ther, 2018, 9: 107 PMID: 29661222
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Arum Park, .et al. Identification of Transcription Factor YY1 as a Regulator of a Prostate Cancer-Specific Pathway Using Proteomic Analysis, J Cancer, 2017, 8(12): 2303-2311 PMID: 28819434
- Cong Li, .et al. AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia., Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Zhihong Li, .et al. Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3, J Med Chem, 2014, Apr 24;57(8):3430-49 PMID: 24641103
- Hideki Yamaguchi, .et al. Saracatinib impairs the peritoneal dissemination of diffuse-type gastric carcinoma cells resistant to Met and fibroblast growth factor receptor inhibitors, Cancer Sci, 2014, 105(5): 528-536 PMID: 24612061
- Yaping Zhang, .et al. FLT3 and CDK4/6 inhibitors: Signaling mechanisms and tumor burden in subcutaneous and orthotopic mouse models of acute myeloid leukemia, J Pharmacokinet Pharmacodyn., 2014, 41(6): 675-691 PMID: 25326874
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Nintedanib esylate

Catalog No. A16197
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RTK 抑制剂

Nintedanib esylate是多种受体酪氨酸激酶（RTK）和非受体酪氨酸激酶（nRTK）的有效抑制剂。了解更多

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- Thibaut Fourniols, .et al. Inhibition of Colorectal Cancer-Associated Fibroblasts by Lipid Nanocapsules Loaded With Acriflavine or Paclitaxel, Int J Pharm, 2020, Jun 30;584:119337 PMID: 32371002
- 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
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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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