FGFR1 Inhibitor

FGFR1 Inhibitors (91):

Cat. No.	Product Name	Effect	Purity

HY-100491

H3B-6527	Inhibitor	≥98.0%
H3B-6527 is an orally active, highly selective and covalent FGFR4 inhibitor with an IC₅₀ of <1.2 nM. H3B-6527 has at least 250-fold selectivity over FGFR1-3 with IC₅₀s of 320 nM, 1290 nM and 1060 nM respectively. H3B-6527 has potent anti-cancer activity.

HY-15599

SSR128129E	Inhibitor	99.85%
SSR128129E is an orally available and allosteric FGFR inhibitor with an IC₅₀ of 1.9 μM for FGFR1.

HY-100434

PD-161570	Inhibitor	99.82%
PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC₅₀ of 39.9 nM and a K_i of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC₅₀ values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC₅₀s of 450 nM and 622 nM, respectively. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor.

HY-101466

E7090	Inhibitor	99.64%
E7090 is an orally available, potent, and selective FGFR inhibitor with IC₅₀s of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/FGFR2/FGFR3/FGFR4, respectively.

HY-156019

FGFR1 inhibitor-10	Inhibitor	98.92%
FGFR1 inhibitor-10 (Compound 4i) is an FGFR1 inhibitor (IC₅₀: 28 nM). FGFR1 inhibitor-10 inhibits the phosphorylation of FGFR1. FGFR1 inhibitor-10 has anti-angiogenic, anti-invasion activity, and anti-tumor effect.

HY-15813

FIIN-1	Inhibitor	99.11%
FIIN-1 is a potent, irreversible, selective FGFR inhibitor. FIIN-1 binds to FGFR1/2/3/4 and Flt1/4 with K_ds of 2.8/6.9/5.4/120 nM and 32/120 nM respectively. The biochemical IC₅₀s of FIIN-1 are 9.2, 6.2, 11.9, and 189 nM against FGFR1/2/3/4, respectively.

HY-10186

TG 100801	Inhibitor	98.61%
TG 100801 is a proagent that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC₅₀s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1/Flt-1, VEGFR2/KDR/Flk-1, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.

HY-118203

SU4984	Inhibitor	99.14%
SU4984 is a protein tyrosine kinase inhibitor, with an IC₅₀ of 10-20 μM for fibroblast growth factor receptor 1 (FGFR1). SU4984 is also inhibits platelet-derived growth factor receptor, and insulin receptor. SU4984 can be used for the research of cancer.

HY-16025

EOC317	Inhibitor	98.05%
EOC317 (ACTB-1003) is an oral kinase inhibitor with IC₅₀s of 6, 2 and 4 nM for FGFR1, VEGFR2/KDR/Flk-1 and Tie-2.

HY-18603

FIIN-3	Inhibitor	99.66%
FIIN-3 is an irreversible inhibitor of FGFR with an IC₅₀ of 13.1, 21, 31.4, and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.

HY-159642

TYRA-300	Inhibitor	99.90%
TYRA-300 is an orally active, selective inhibitor for FGFR3 with an IC₅₀ of 11 nM in Ba/F3. TYRA-300 exhibits antitumor efficacy against urothelial cancers and solid tumors.

HY-10987

ENMD-2076 Tartrate	Inhibitor	99.42%
ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC₅₀s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, VEGFR2/KDR/Flk-1/VEGFR2/KDR/Flk-1, Flt4/VEGFR3/Flt-4, FGFR1, FGFR2, Src, PDGFRα, respectively.

HY-10185

TG 100572 Hydrochloride	Inhibitor	98.96%
TG 100572 Hydrochloride is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC₅₀s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1/Flt-1, VEGFR2/KDR/Flk-1, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.

HY-10207

Dovitinib lactate	Inhibitor	99.75%
Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC₅₀s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/Flt-1/2/3 and PDGFRα/β, respectively.

HY-131908

CPL304110	Inhibitor	99.85%
CPL304110 is a potent, orally active and selective inhibitor of fibroblast growth factor receptors FGFR (1-3), with IC₅₀ values of 0.75 nM, 0.5 nM, and 3.05 nM for FGFR (1-3), respectively.

HY-108933

JK-P3	Inhibitor	99.72%
JK-P3 is a potent and pan VEGFR2/KDR/Flk-1 inhibitor, with IC₅₀s of 7.83 μM, 27 μM and 5.18 μM for VEGFR2/KDR/Flk-1, FGFR1 and FGFR3, respectively. JK-P3 can inhibit VEGF-A-stimulated VEGFR2/KDR/Flk-1 activation and intracellular signalling, also inhibits endothelial monolayer wound closure and angiogenesis, as well as fibroblast growth factor receptor kinase activity in vitro. JK-P3 has anti-angiogenic activity.

HY-13737

R1530	Inhibitor	99.06%
R1530 is a highly potent, orally active, dual-acting mitosis/angiogenesis inhibitor, with anti-tumor and anti-angiogenic activities. R1530 is a multikinase inhibitor which binds to 31 kinases with K_d values of <500 nM. R1530 inhibits VGFR2 and FGFR1 with IC₅₀ of 10 nM and 28 nM, respectively. R1530 triggers apoptosis (mitotic catastrophe) or senescence.

HY-112345

PD-089828	Inhibitor	98.07%
PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC₅₀s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC₅₀=0.18 µM). PD-089828 also inhibits MAPK with an IC₅₀ of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity.

HY-10517A

(Z)-Orantinib	Inhibitor	99.44%
(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/VEGFR2/KDR/Flk-1, PDGFRβ, and FGFR1, with IC₅₀s of 2.1, 0.008, and 1.2 µM, respectively. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces regression of established tumors.

HY-12965

S49076	Inhibitor	99.44%
S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC₅₀ values below 20 nM.

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