FGFR Inhibitors

FGFR

FGFR1

FGFR2

FGFR3

FGFR4

FGF21

FGFR Inhibitors, Agonists & Activators

Product Name	FGFR	FGFR1	FGFR2	FGFR3	FGFR4	FGF21	Purity
Lenvatinib		FGFR1, IC₅₀: 46 nM					99.84%
Nintedanib		FGFR1, IC₅₀: 69 nM	FGFR2, IC₅₀: 37 nM	FGFR3, IC₅₀: 108 nM			99.94%
Ponatinib		FGFR1, IC₅₀: 2.2 nM					99.43%
Erdafitinib		FGFR1, IC₅₀: 1.2 nM	FGFR2, IC₅₀: 2.5 nM	FGFR3, IC₅₀: 3.0 nM	FGFR4, IC₅₀: 5.7 nM		99.66%
H3B-6527		FGFR1, IC₅₀: 320 nM	FGFR2, IC₅₀: 1290 nM	FGFR3, IC₅₀: 1060 nM	FGFR4, IC₅₀: <1.2 nM		≥98.0%
Infigratinib		FGFR1, IC₅₀: 0.9 nM	FGFR2, IC₅₀: 1.4 nM	FGFR3, IC₅₀: 1 nM	FGFR4, IC₅₀: 60 nM		99.72%
Pemigatinib		FGFR1, IC₅₀: 0.4 nM	FGFR2, IC₅₀: 0.5 nM	FGFR3, IC₅₀: 1.2 nM	FGFR4, IC₅₀: 30 nM		99.73%
Pazopanib		FGFR1, IC₅₀: 140 nM					99.91%
Futibatinib		FGFR1, IC₅₀: 3.9 nM	FGFR2, IC₅₀: 1.3 nM wild-type FGFR2, IC₅₀: 0.3 nM FGFR2 V5651, IC₅₀: 1-3 nM FGFR2 N550H, IC₅₀: 3.6 nM FGFR2 E566G, IC₅₀: 2.4 nM	FGFR3, IC₅₀: 1.6 nM	FGFR4, IC₅₀: 8.3 nM		99.65%
Fexagratinib		FGFR1, IC₅₀: 0.2 nM	FGFR2, IC₅₀: 2.5 nM	FGFR3, IC₅₀: 1.8 nM	FGFR4, IC₅₀: 165 nM		99.85%
Formononetin			FGFR2, IC₅₀: 4.31 μM				99.92%
PD173074		FGFR1, IC₅₀: 25 nM					99.70%
SU 5402		FGFR1, IC₅₀: 30 nM					99.38%
Nintedanib esylate		FGFR1, IC₅₀: 69 nM	FGFR2, IC₅₀: 37 nM	FGFR3, IC₅₀: 108 nM			99.95%
Lenvatinib mesylate		FGFR1, IC₅₀: 46 nM					99.86%
Dovitinib		FGFR1, IC₅₀: 8 nM		FGFR3, IC₅₀: 9 nM			99.94%
KW-2449		FGFR1, IC₅₀: 36 nM					99.69%
Ferulic acid		FGFR1, IC₅₀: 3.78 μM	FGFR2, IC₅₀: 12.5 μM				99.87%
PD-166866		FGFR1, IC₅₀: 52.4 nM					99.89%
Fisogatinib					FGFR4, IC₅₀: 5 nM		99.87%
Gandotinib			FGFR2, IC₅₀: 32 nM	FGFR3, IC₅₀: 106 nM			99.82%
BLU9931		FGFR1, IC₅₀: 591 nM	FGFR2, IC₅₀: 493 nM	FGFR3, IC₅₀: 150 nM	FGFR4, IC₅₀: 3 nM		99.95%
Roblitinib		FGFR1, IC₅₀: >10 μM	FGFR2, IC₅₀: >10 μM	FGFR3, IC₅₀: >10 μM	FGFR4, IC₅₀: 1.9 nM rat FGFR4, IC₅₀: >10 μM		99.74%
Pazopanib Hydrochloride		FGFR1, IC₅₀: 140 nM					99.88%
Sulfatinib		FGFR1					98.65%
LY2874455		FGFR1, IC₅₀: 2.8 nM	FGFR2, IC₅₀: 2.6 nM	FGFR3, IC₅₀: 6.4 nM	FGFR4, IC₅₀: 6 nM		98.03%
Rogaratinib		FGFR1	FGFR2	FGFR3	FGFR4		99.86%
Lirafugratinib			FGFR2, IC₅₀: 3 nM				99.60%
Ponatinib hydrochloride		FGFR1, IC₅₀: 2.2 nM					99.55%
Efruxifermin						FGF21	98.32%
Surfen dihydrochloride			FGFR2, IC₅₀: 5 μM				≥99.0%
Orantinib		FGFR1, Ki: 1.2 μM					99.21%
Lucitanib		FGFR1, IC₅₀: 17.5 nM	FGFR2, IC₅₀: 82.5 nM				98.94%
Alofanib			FGFR2				99.90%
PF 477736				FGFR3, IC₅₀: 23 nM			99.21%
ENMD-2076		FGFR1, IC₅₀: 92.7 nM	FGFR2, IC₅₀: 70.8 nM				99.12%
CP-547632	FGFR, IC₅₀: 9 nM						99.16%
ODM-203		FGFR1, IC₅₀: 11 nM	FGFR2, IC₅₀: 16 nM	FGFR3, IC₅₀: 6 nM	FGFR4, IC₅₀: 35 nM		99.91%
Zoligratinib		FGFR1, IC₅₀: 9.3 nM	FGFR2, IC₅₀: 7.6 nM	FGFR3, IC₅₀: 22 nM	FGFR4, IC₅₀: 290 nM		99.76%
ASP5878		FGFR1, IC₅₀: 0.47 nM	FGFR2, IC₅₀: 0.6 nM	FGFR3, IC₅₀: 0.74 nM	FGFR4, IC₅₀: 3.5 nM		99.86%
SSR128129E		FGFR1, IC₅₀: 1.9 μM					99.85%
Infigratinib phosphate		FGFR1, IC₅₀: 0.9 nM	FGFR2, IC₅₀: 1.4 nM	FGFR3, IC₅₀: 1 nM	FGFR4, IC₅₀: 60 nM		99.74%
PRN1371		FGFR1, IC₅₀: 0.6 nM	FGFR2, IC₅₀: 1.3 nM	FGFR3, IC₅₀: 4.1 nM	FGFR4, IC₅₀: 19.3 nM		99.43%
CP-547632 hydrochloride	FGFR, IC₅₀: 9 nM						99.88%
Derazantinib		FGFR1, IC₅₀: 4.5 nM	FGFR2, IC₅₀: 1.8 nM	FGFR3, IC₅₀: 4.5 nM			99.28%
Vofatamab				FGFR3
FIIN-2		FGFR1, IC₅₀: 3.1 nM	FGFR2, IC₅₀: 4.3 nM	FGFR3, IC₅₀: 27 nM	FGFR4, IC₅₀: 45 nM		99.63%
Aprutumab			FGFR2-IIIb FGFR2-IIIc
Dovitinib lactate		FGFR1, IC₅₀: 8 nM		FGFR3, IC₅₀: 9 nM			99.62%
FGFR2-IN-2		FGFR1, IC₅₀: 389 nM	FGFR2, IC₅₀: 29 nM	FGFR3, IC₅₀: 758 nM			98.09%
TG 100572 Hydrochloride		FGFR1, IC₅₀: 2 nM	FGFR2, IC₅₀: 16 nM				98.96%
Lirafugratinib hydrochloride			FGFR2, IC₅₀: 3 nM				98.73%
FGFR3-IN-5		FGFR1, IC₅₀: 289 nM	FGFR2, IC₅₀: 44 nM	FGFR3, IC₅₀: 3 nM			99.28%
Tyrosine kinase-IN-1		FGFR1, IC₅₀: 2 nM					99.34%
ENMD-2076 Tartrate		FGFR1, IC₅₀: 92.7 nM	FGFR2, IC₅₀: 70.8 nM				99.42%
FGFR1/DDR2 inhibitor 1		FGFR1, IC₅₀: 31.1 nM					98.26%
E7090		FGFR1, IC₅₀: 0.71 nM	FGFR2, IC₅₀: 0.50 nM	FGFR3, IC₅₀: 1.2 nM	FGFR4, IC₅₀: 120 nM		99.64%
CPL304110		FGFR1, IC₅₀: 0.75 nM	FGFR2, IC₅₀: 0.5 nM	FGFR3, IC₅₀: 3.05 nM			99.68%
TG 100801		FGFR1, IC₅₀: 2 nM	FGFR2, IC₅₀: 16 nM				98.60%
Gunagratinib	FGFR						99.36%
R1530		FGFR1, IC₅₀: 28 nM					99.06%
FIIN-1		FGFR1, Kd: 2.8 nM FGFR1, IC₅₀: 9.2 nM	FGFR2, Kd: 6.9 nM FGFR2, IC₅₀: 6.2 nM	FGFR3, Kd: 5.4 nM FGFR3, IC₅₀: 11.9 nM	FGFR4, Kd: 120 nM FGFR4, IC₅₀: 189 nM		99.11%
SU4984		FGFR1, IC₅₀: 10-20 μM					99.14%
EOC317		FGFR1, IC₅₀: 6 nM					98.05%
S49076		FGFR1, IC₅₀: 18 nM FGFR1^V561M, IC₅₀: 23 nM	FGFR2, IC₅₀: 17 nM FGFR2^N549H, IC₅₀: 19 nM	FGFR3, IC₅₀: 15 nM			99.71%
FGFR1 inhibitor-10		FGFR1					98.92%
PD-089828		FGFR1, IC₅₀: 0.15 μM FGFR1, Ki: 0.14 μM					98.07%
FIIN-3		FGFR1, IC₅₀: 13.1 nM	FGFR2, IC₅₀: 21 nM	FGFR3, IC₅₀: 31.4 nM	FGFR4, IC₅₀: 35.3 nM		99.66%
FGFR4-IN-5			FGFR2, IC₅₀: 505 nM		FGFR4, IC₅₀: 6.5 nM		98.03%
VSPPLTLGQLLS				FGFR3 K650M-FGFR3 K644E FGFR3			98.08%
Fazpilodemab		FGFR1c					99.00%
Recifercept				FGFR3
JK-P3		FGFR1, IC₅₀: 27 μM		FGFR3, IC₅₀: 5.18 μM			99.72%
(Z)-Orantinib		FGFR1, IC₅₀: 1.2 μM					99.02%
LC-MB12			FGFR2, DC₅₀: 11.8 nM				99.23%
CP-547632 TFA	FGFR, IC₅₀: 9 nM						99.42%
TG 100572		FGFR1, IC₅₀: 2 nM	FGFR2, IC₅₀: 16 nM
Dovitinib lactate hydrate		FGFR1, IC₅₀: 8 nM		FGFR3, IC₅₀: 9 nM
E7090 succinate		FGFR1, IC₅₀: 0.71 nM	FGFR2, IC₅₀: 0.50 nM	FGFR3, IC₅₀: 1.2 nM	FGFR4, IC₅₀: 120 nM		99.17%
FGFR4-IN-11					FGFR4, IC₅₀: 2.1 nM
FGFR4-IN-4					FGFR4
FGFR1 inhibitor-2		FGFR1
ARQ 069		unphosphorylated FGFR1, IC₅₀: 0.84 μM FGFR1 autophosphorylation, IC₅₀: 2.8 μM	unphosphorylated FGFR2, IC₅₀: 1.23 μM FGFR2 autophosphorylation, IC₅₀: 1.9 μM
FGFR3-IN-6				FGFR3
FGFR-IN-2		FGFR1, IC₅₀: 7.3 nM	FGFR2, IC₅₀: 4.3 nM	FGFR3, IC₅₀: 7.6 nM	FGFR4, IC₅₀: 11 nM
FGFR3-IN-4				FGFR3, IC₅₀: < 50 nM
FGFR-IN-9		FGFR1, IC₅₀: 64.3 nM	FGFR2, IC₅₀: 46.7 nM	FGFR3, IC₅₀: 29.6 nM	FGFR4^WT, IC₅₀: 17.1 nM FGFR4^V550L, IC₅₀: 30.7 nM
FGFR-IN-8		FGFR1, IC₅₀: <0.5 nM V561M-FGFR1, IC₅₀: 262.5 nM	V564F-FGFR2, IC₅₀: 189.1 nM N549H-FGFR2, IC₅₀: <0.5 nM	V555M-FGFR3, IC₅₀: 22.6 nM FGFR3, IC₅₀: <0.5 nM K650E-FGFR3, IC₅₀: <0.5 nM K650M-FGFR3, IC₅₀: 4.8 nM	FGFR4, IC₅₀: 7.30 nM
FGFR3-IN-2				FGFR3, IC₅₀: 4.1 nM
FGFR-IN-10			FGFR2, IC₅₀: 104.1 nM V564F-FGFR2, IC₅₀: 43.6 nM
FGFR4-IN-10					FGFR4, IC₅₀: 70.7 nM
FGFR3-IN-7				FGFR3
CXF-009					FGFR4, IC₅₀: 48 nM
FGFR2/3-IN-1		FGFR1, IC₅₀: 21 nM	FGFR2, IC₅₀: 1 nM	FGFR3, IC₅₀: 0.5 nM FGFR3 V555L, IC₅₀: 2.7 nM FGFR3 V555M, IC₅₀: 6.1 nM	FGFR4, IC₅₀: 145 nM
FGFR2-IN-1			FGFR2, IC₅₀: 140 nM				99.78%
Picrasidine Q			FGFR2
FGFR-IN-11		FGFR1, IC₅₀: 9.9 nM	FGFR2, IC₅₀: 3.1 nM	FGFR3, IC₅₀: 16 nM	FGFR4, IC₅₀: 1.8 nM
3-Methylthienyl-carbonyl-JNJ-7706621			FGFR2, IC₅₀: 0.22 μM
Multi-kinase-IN-2		FGFR1, IC₅₀: 23 ± 2.5 nM
FGFR4-IN-9					FGFR4, IC₅₀: 75.3 nM
Multi-kinase-IN-5		FGFR1, IC₅₀: 1.287 μM
HDAC-IN-50		FGFR1, IC₅₀: 0.18 nM	FGFR2, IC₅₀: 1.2 nM	FGFR3, IC₅₀: 0.46 nM	FGFR4, IC₅₀: 1.4 nM
FGFR1 inhibitor-6		FGFR1, IC₅₀: 16.31 nM
VSPPLTLGQLLS TFA				FGFR3 K650M-FGFR3 K644E FGFR3
FGFR3-IN-3		FGFR1, IC₅₀: 2.1 nM	FGFR2, IC₅₀: 3.1 nM	FGFR3, IC₅₀: 4.3 nM	FGFR4, IC₅₀: 74 nM
FGFR3-IN-1		FGFR1, IC₅₀: 40 nM	FGFR2, IC₅₀: 5.1 nM	FGFR3, IC₅₀: 12 nM
CXF-007					FGFR4, IC₅₀: 7 nM
TG 100801 Hydrochloride		FGFR1, IC₅₀: 2 nM	FGFR2, IC₅₀: 16 nM
SSR128129E free acid		FGFR1, IC₅₀: 1.9 μM

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