FGFR Inhibitor

PRX-08066 is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a K_i of 3.4 nM. PRX-08066 inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 inhibits pulmonary vascular remodeling. PRX-08066 can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET).

FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC₅₀ values of 31.1 nM and 3.2 nM, respectively. Antitumor activity.

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, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.

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.

Lirafugratinib (RLY-4008) hydrochloride is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC₅₀ of 3 nM. Lirafugratinib hydrochloride covalently binds to Cys491. Lirafugratinib hydrochloride targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs.

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.

XL999 is a multi-target tyrosine kinase inhibitor. XL999 has IC₅₀ values for KDR, Flt-1, FGFR1 and PDGFRα of 4 nM, 20 nM, 4 nM and 2 nM, respectively. XL999 can be used in the research of cancer.

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, VEGFR1/2/3 and PDGFRα/β, respectively.

CP-547632 hydrochloride is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC₅₀s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 hydrochloride has antitumor efficacy.

Aprutumab ixadotin (BAY 1187982) is the first antibody-drug conjugate (ADC) to target FGFR2 and the first to use Auristatin-based payload. Aprutumab ixadotin contains a fully human anti-FGFR2 monoclonal antibody (Aprutumab) (HY-P99007) conjugated by lysine side chains to a non-cleavable linker and via this an innovative Auristatin W derivative. Aprutumab ixadotin can be used for the study of advanced solid tumors, such as FGFR2-positive gastric cancer and triple-negative breast cancer.

2,5-Dihydroxybenzoic acid (Standard) is the analytical standard of 2,5-Dihydroxybenzoic acid. This product is intended for research and analytical applications. 2,5-Dihydroxybenzoic acid is a derivative of benzoic and a powerful inhibitor of fibroblast growth factors.

S6K2-IN-1 (Compound 2) is a S6K2 inhibitor (IC₅₀: 22 nM). S6K2-IN-1 also inhibits FGFR4 (IC₅₀: 216 nM). S6K2-IN-1 has acceptable stability in mouse liver microsomes.

FGFR2-IN-1 is a selective FGFR2 inhibitor with an IC₅₀ of 140 nM.

Formononetin (Standard) is the analytical standard of Formononetin. This product is intended for research and analytical applications. Formononetin is a potent FGFR2 inhibitor with an IC50 of ~4.31 μM. Formononetin potently inhibits angiogenesis and tumor growth.

EOC317 (ACTB-1003) is an oral kinase inhibitor with IC₅₀s of 6, 2 and 4 nM for FGFR1, VEGFR2 and Tie-2.

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.

FGFR4-IN-1 (example 98) is a potent inhibitor of FGFR4 with IC₅₀ of 0.4 nM.

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.

Nintedanib-d₈ is deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

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