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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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

Product Citations (1)

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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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FIIN-3

Catalog No. A15848
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Irreversible FGFR 抑制剂

FIIN-3是一种有效的，选择性的，不可逆的下一代共价FGFR抑制剂。了解更多

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- Li Tan,etc. Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proc Natl Acad Sci USA. 2014 Nov 11; 111(45): E4869–E4877.
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AZD4547

Catalog No. A11075
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FGFR 抑制剂

AZD4547是一种有效，选择性和口服活性的pan-FGFR抑制剂，对于FGFR1、2、3和4的IC50分别为0.2、2.5、1.8和165 nM。了解更多

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- Ryuma Tokunaga, .et al. Fibroblast growth factor receptor 2 expression, but not its genetic amplification, is associated with tumor growth and worse survival in esophagogastric junction adenocarcinoma, Oncotarget, 2016, Apr 12; 7(15): 19748-19761 PMID: 26933914
- Mitsuko Kawano, .et al. FGF18 signaling in the hair cycle resting phase determines radioresistance of hair follicles by arresting hair cycling, Adv Radiat Oncol, 2016, Jul-Sep; 1(3): 170-181 PMID: 28740887
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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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BGJ398 (NVP-BGJ398)

Catalog No. A11159
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FGFR 抑制剂

BGJ398 (NVP-BGJ398)是一种有效的选择性抑制剂，具有成纤维细胞生长因子受体（FGFR）酪氨酸激酶1、2、3和4的潜在抗血管生成和抗肿瘤活性（对于FGFR1，FGFR2，FGFR3，IC50值为0.9、1.4、1.0和60 nM，和FGFR4）。了解更多

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- Takehito Yamamoto, .et al. Chemosensitivity of Patient-Derived Cancer Stem Cells Identifies Colorectal Cancer Patients with Potential Benefit from FGFR Inhibitor Therapy, Cancers (Basel), 2020, Jul 22;12(8):E2010 PMID: 32708005
- Daniel Limonta, .et al. Fibroblast growth factor 2 enhances Zika virus infection in human fetal brain, J Infect Dis, 2019, 2019 PMID: 30799482
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Anil Kumar, .et al. Human Sertoli cells support high levels of Zika virus replication and persistence, Sci Rep, 2018, 8: 5477 PMID: 29615760
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XL-228

Catalog No. A13069
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IGF-1R, Aurora, FGFR, ABL, SRC 抑制剂

XL228是靶向IGF1R，AURORA激酶，FGFR1-3，ABL和SRC家族激酶的蛋白激酶抑制剂。XL228是一种Aurora A抑制剂（IC50，f3 nmol/L），对ABL1（Ki，5 nmol/L）以及BCR-ABL1 T315I（Ki，1.4 nmol/L）激酶显示出有效的生化活性。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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BLU9931

Catalog No. A15534
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FGFR 抑制剂

BLU9931是第一种选择性的FGFR4小分子抑制剂，IC50为3 nM。对FGFR1/2/3的效力较低（IC50> 150 nM）。了解更多

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Debio-1347 (CH5183284)

Catalog No. A14415
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FGFR1/2/3 抑制剂

Debio-1347 (CH5183284)是成纤维细胞生长因子受体亚型1（FGFR-1），2（FGFR-2）和3（FGFR-3）的生物利用抑制剂，具有潜在的抗肿瘤活性。了解更多

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LY 2874455

Catalog No. A11244
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FGFR/VEGFR2 抑制剂

LY2874455是一种新型有效的FGFR / VEGFR抑制剂。了解更多

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FIIN-2

Catalog No. A12357
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FGFR 抑制剂

FIIN-2是FGFR1-4的不可逆抑制剂，IC50值分别为3.1、4.3、27和45 nM。了解更多

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NVP-BGJ398 phosphate

Catalog No. A15194
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FGFR 抑制剂

NVP-BGJ398 phosphate是一种新型的选择性泛特异性FGFR抑制剂，对FGFR1，FGFR2和FGFR3的IC50分别为0.9、1.4和1 nM。与FGFR4和VEGFR2相比，对FGFR具有40倍以上的选择性，并且对Abl，Fyn，Kit，Lck，Lyn和Yes的活性很小。了解更多

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