FGFR

Inhibitory Selectivity

Catalog No.	Inhibitor Name	FGFR	FGFR1	FGFR2	FGFR3	FGFR4	Other
A10080	Ponatinib		****				Abl,PDGFRα,VEGFR2
A11159	BGJ398		****	****	****	**	VEGFR2,Lyn,Kit
A10137	Nintedanib		**	**	**	*	VEGFR3,VEGFR2,LCK
A10703	PD173074		**				VEGFR2,c-Src
A11411	Dovitinib		***		***		FLT3,c-Kit,VEGFR3/FLT4
A11075	AZD4547		****	****	****	*	KDR,IGFR
A10715	Danusertib		**				Aurora A,Abl,TrkA
A10953	Orantinib		*				PDGFRβ,Flk1
A10254	Brivanib		*				VEGFR2,Flk1,VEGFR1
A10198	Dovitinib Dilactic Acid		***		***		FLT3,c-Kit,VEGFR3/FLT4
A11753	MK-2461		**	**	**
A10162	Brivanib Alaninate		*				VEGFR2,Flk1,VEGFR1
A13211	SSR128129E		*				VEGFR2,PDGFRβ
A11558	SU5402		**
A15534	BLU9931		*	*	*	****
A12357	FIIN-2		****	***	**	**	FLT3,c-Kit,VEGFR3/FLT4
A14415	CH5183284		***	***	***	*	VEGFR2
A11244	LY2874455		****	****	***	***
A15957	Erdafitinib
A10508	KW-2449		**				FLT3, Bcr-Abl, Aurora A, PDGFRβ, IGF-1R, EGFR
A10699	Pazopanib HCl	*					VEGFR1, VEGFR2, VEGFR3, PDGFR, c-Kit, c-Fms
A11518	Pazopanib	*					VEGFR1, VEGFR2, VEGFR3, PDGFR, c-Kit, c-Fms
A13111	R 1530		*				Chk2, KDR, FGFR, Aurora A, Cdk2, VEGFR-2, PDGFRβ
A15073	E-3810		***	**			VEGFR1, VEGFR2, VEGFR3
A15848	FIIN-3		***	**	**	**
A15957	Alofanib (RPT835)

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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TSU-68 (Orantinib, SU6668)

Catalog No. A10953
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PDFGRβ 抑制剂

TSU-68 (Orantinib,SU6668)在无细胞试验中具有8 nM的Ki对PDGFR自磷酸化的最大效力，但也强烈抑制Flk-1和FGFR1反磷酸化，对IGF-1R，Met，Src， Lck，Zap70，Abl和CDK2；不抑制EGFR。了解更多

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- Aaron Y. Lai, .et al. Venular degeneration leads to vascular dysfunction in a transgenic model of Alzheimer's disease., Brain, 2015, Apr;138(Pt 4):1046-58 PMID: 25688079
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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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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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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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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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