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.

Catalog No.	Product Name	Application	Product Information
A11411 SALE	Dovitinib (TKI-258)	RTK inhibitor	Dovitinib is a small-molecule multitargeted receptor tyrosine kinase inhibitor, which inhibits Ba/F3 cells transformed to IL3 independence by ZNF198-FGFR1 or BCR-FGFR1 with IC50 values of 150 nM and 90 nM, respectively. Product Citations (1) Samuel Q. Li, etc. Targeting Wild-Type and Mutationally Activated FGFR4 in Rhabdomyosarcoma with the Inhibitor Ponatinib (AP24534). PLoS One. 2013; 8(10): e76551.
A13069 SALE	XL-228	IGF-1R, Aurora, FGFR, ABL, SRC inhibitor	XL228 is a protein kinase inhibitor targeting IGF1R, the AURORA kinases, FGFR1-3, ABL and SRC family kinases. XL228 is an Aurora A inhibitor (IC50, f3 nmol/L) that has shown potent biochemical activity against ABL1 (Ki, 5 nmol/L), as well as the BCR-ABL1 T315I (Ki, 1.4 nmol/L) kinases.
A13111 SALE	R1530	Chk2, KDR, FGFR, Aurora A & Cdk2 inhibitor	R1530 is a pyrazolobenzodiazepine small molecule with potential antiangiogenesis and antineoplastic activities. R1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta? FMS-like tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2.
A13211	SSR128129E	FGFR1 inhibitor	SSR128129E is an orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 uM
A14415	Debio-1347 (CH5183284)	FGFR1/2/3 inhibitor	Debio-1347 is an orally bioavailable inhibitor of the fibroblast growth factor receptor subtypes 1 (FGFR-1), 2 (FGFR-2) and 3 (FGFR-3), with potential antineoplastic activity.
A14431 SALE	ACTB-1003	FGFR1 inhibitor	ACTB-1003 is an oral kinase inhibitor targeting cancer mutations (FGFR inhibition), angiogenesis (inhibition of VEGFR2 and Tie-2) and induces apoptosis (targeting RSK and p70S6K, downstream of PI3 kinase).
A15073	E-3810	VEGFR/FGFR Inhibitor	E-3810 is a potent and selective dual inhibitor of VEGF and FGF receptors with IC50 values of 7 nM, 25 nM, 10 nM, 17.5 nM and 82.5 nM for VEGFR-1, VEGFR-2, VEGFR-3, FGFR-1 and FGFR-2, respectively.
A15194	NVP-BGJ398 phosphate	FGFR Inhibitor	NVP-BGJ398 phosphate is a novel selective, pan-specific FGFR inhibitor with IC50 of 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively; >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes.
A15534 SALE	BLU9931	FGFR inhibitor	BLU9931 is the first selective small molecule inhibitor of FGFR4 with IC50 of 3 nM; less potent for FGFR1/2/3(IC50> 150 nM),
A12357 SALE	FIIN-2	FGFR Inhibitor	FIIN-2 is an irreversible inhibitor of FGFR1-4 with IC50 values of 3.1, 4.3, 27, and 45 nM, respectively.
A15848	FIIN-3	Irreversible FGFR inhibitor	FIIN-3 is a potent, selective, irreversible and the next-generation covalent FGFR inhibitor. Product Citations (1) 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.
A15946	Alofanib (RPT835)	FGFR2 Inhibitor	Alofanib is a potent and selective allosteric inhibitor of FGFR2 with potential anticancer activity.
A15957	Erdafitinib (JNJ-42756493)	FGFR inhibitor	Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity.
A16197	Nintedanib esylate	RTK inhibitor	Nintedanib is a potent inhibitor of multiple receptor tyrosine kinases (RTKs) and non-receptor tyrosine kinases (nRTKs).
A16251	FGFR4-IN-1	FGFR4 inhibitor	FGFR4-IN-1 is a potent inhibiotr of FGFR4 with IC50 of 0.7 nM.
A11558 SALE	SU-5402	VVEGFR/FGFR/EGFR inhibitor‎	SU-5402 is a potent and selective vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) inhibitor (IC50 values are 0.02, 0.03, 0.51 and > 100 μM at VEGFR2, FGFR1, PDGFRβ and EGFR respectively). Product Citations (1) 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.
A11244 SALE	LY 2874455	FGFR/VEGFR2 inhibitor	LY2874455 is a novel and potent FGFR/VEGFR Inhibitor.
A10080 SALE	AP24534 (Ponatinib)	BCR-ABL inhibitor	AP24534 (Ponatinib) is a potent multi-kinase and pan-BCR-ABL inhibitor. Product Citations (5) Yamamoto Y, .et al. Development of a sandwich enzyme-linked immunosorbent assay for the quantification of ponatinib in serum, Anal Biochem, 2019, Feb 13. pii: S0003-2697(18)31083-2 PMID: 30771339 N Naganna, .et al. Amino alkynylisoquinoline and alkynylnaphthyridine compounds potently inhibit acute myeloid leukemia proliferation in mice, EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755 Takuya Hirao, .et al. Altered intracellular signaling by imatinib increases the anti-cancer effects of tyrosine kinase inhibitors in chronic myelogenous leukemia cells, Cancer Sci, 2018, Jan; 109(1): 121-131 PMID: 29121435 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 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
A10715 SALE	Danusertib (PHA-739358)	Aurora inhibitor	Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2 Product Citations (1) Samuel Q. Li, etc. Targeting Wild-Type and Mutationally Activated FGFR4 in Rhabdomyosarcoma with the Inhibitor Ponatinib (AP24534). PLoS One. 2013; 8(10): e76551.
A10137 SALE	Bibf1120 (Vargatef)	VEGFR inhibitor	BIBF1120 (Vargatef) is a novel triple angiokinase inhibitor that inhibits three growth factor receptors simultaneously: VEGFR, PDGF and FGFR. Product Citations (2) Samuel Q. Li, etc. Targeting Wild-Type and Mutationally Activated FGFR4 in Rhabdomyosarcoma with the Inhibitor Ponatinib (AP24534). PLoS One. 2013; 8(10): e76551. A Sikora ,etc. BIBF 1120 w terapii angiogennej nowotworów. Porównanie szybkości uwalniania pantoprazolu z tabletek dojelitowych i układów wielozbiornikowych, 2014, 70(5), 235-239.
A10703 SALE	PD173074	FGFR1/VEGFR2 Inhibitor	PD173074 is a potent, cell permeable and ATP competitive inhibitor of FGFR and VEGFR. Product Citations (1) Cheryl Q.E. Lee, .et al. What Is Trophoblast? A Combination of Criteria Define Human First-Trimester Trophoblast, Stem Cell Reports, 2016, Feb 9; 6(2): 257-272 PMID: 26862703
A10953 SALE	TSU-68 (Orantinib, SU6668)	PDFGRβ inhibitor	Orantinib (TSU-68, SU6668) has greatest potency against PDGFR autophosphorylation with Ki of 8 nM in a cell-free assay, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does not inhibit EGFR. Phase 3. Product Citations (1) 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
A10254 SALE	Brivanib (BMS-540215)	VEGFR-2 inhibitor	Brivanib (BMS-540215) is a VEGFR -2 inhibitor with an IC50 of 25 nM and Ki of 26 nM. Product Citations (1) Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
A10162	Brivanib alaninate (BMS-582664)	VEGFR inhibitor	Brivanib alaninate (BMS-582664) is a dual tyrosine kinase inhibitor of VEGFR and FGFR signaling.
A10508 SALE	KW-2449	FLT3/FGFR/Bcr-Abl/Aurora Inhibitor	KW-2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase.
A11075 SALE	AZD4547	FGFR inhibitor	AZD4547 is a potent, selective and orally active pan-FGFR inhibitor, with IC50s of 0.2, 2.5, 1.8 and 165 nM for FGFR1, 2, 3 and 4, respectively. Product Citations (2) 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
A11159 SALE	BGJ398 (NVP-BGJ398)	FGFR Inhibitor	BGJ398 is a potent and selective inhibitor with potential antiangiogenic and antineoplastic activities of fibroblast growth factor receptor (FGFR) tyrosine kinases 1, 2, 3 and 4 (with IC50 values of 0.9, 1.4, 1.0 and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4 respectively). Product Citations (3) 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
A10699 SALE	Pazopanib HCl (GW786034)	VEGFR/PDGFR/FGFR inhibitor	Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis.
A10198 SALE	Dovitinib Dilactic acid (TKI258 Dilactic acid)	RTK inhibitor	Dovitinib is a small-molecule multitargeted receptor tyrosine kinase inhibitor, which inhibits Ba/F3 cells transformed to IL3 independence by ZNF198-FGFR1 or BCR-FGFR1 with IC50 values of 150 nM and 90 nM, respectively.
A11753	MK-2461	c-Met Inhibitor	MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor.
A11518 SALE	Pazopanib (GW-786034)	VEGFR inhibitor	Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis. Product Citations (3) 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
A16252	H3B-6527	FGFR4 inhibitor	H3B-6527 is a highly selective FGFR4 inhibitor with potent antitumour activity in FGF19 amplified cell lines and mice.

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FGFR

A11411 SALE

A13069 SALE

A13111 SALE

A13211

A14415

A14431 SALE

A15073

A15194

A15534 SALE

A12357 SALE

A15848

A15946

A15957

A16197

A16251

A11558 SALE

A11244 SALE

A10080 SALE

A10715 SALE

A10137 SALE

A10703 SALE

A10953 SALE

A10254 SALE

A10162

A10508 SALE

A11075 SALE

A11159 SALE

A10699 SALE

A10198 SALE

A11753

A11518 SALE

A16252

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