FGFR Inhibitor

bFGF (119-126) is a ligand of bFGF. The complex formed by bFGF (119-126) and bFGF can bind to FGFR1, while inhibiting the bFGF-FGFR1 interaction, FGFR1 phosphorylation and downstream signaling pathways. Therefore, bFGF (119-126) induces cell apoptosis and inhibits cell proliferation, migration, angiogenesis and metastasis. When conjugated with a carrier, bFGF (119-126) enhances cellular uptake via FGFR-mediated endocytosis and serves as an effective FGFR-targeted ligand. When used in combination with ultrasound and Doxorubicin (HY-15142A), bFGF (119-126) significantly enhances the inhibitory effect on tumors. bFGF (119-126) is applicable to research related to lung cancer, breast cancer, glioblastoma and ovarian cancer.

Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC₅₀=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC₅₀s=540/800 nM), Lyn (IC₅₀= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity.

Vosoritide (BMN 111) acetate is a natriuretic peptide receptor 2 (NPR2) agonist that acts on the proliferation and differentiation of chondrocytes to promote bone growth.

Bemarituzumab is a humanized IgG1 monoclonal antibody against FGFR2b (a FGF receptor). Bemarituzumab blocks fibroblast growth factors from binding and activating FGFR2b. Bemarituzumab has antitumor activity against gastric and breast cancer.

CP-547632 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 is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 has antitumor efficacy.

Gunagratinib (ICP-192) is a low toxicity and orally active pan-FGFR (fibroblast growth factor receptors) inhibitor that potently and selectively inhibits FGFR activities irreversibly by covalent binding. Gunagratinib can be used for the research of cancer. Gunagratinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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.

CEP-11981(ESK981; BOL 303213X) is an orally active tyrosine kinase inhibitor (TKI), which can target TIE2, VEGFR1-3 and FGFR1, and has potential anti-tumor and anti-angiogenic effects.

Vosoritide (BMN 111) is a modified recombinant CNP (C-type natriuretic peptide) analogue, binds to NPR-B (natriuretic peptide receptor type B) and reduces the activity of FGFR3 (fibroblast growth factor receptor 3). Vosoritide can be used in achondroplasia and dwarfism research.

Bemarituzumab (FUT8-KO) is an anti-FGFR2b monoclonal antibody expressed by CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out. Fucose deficiency enhances the ADCC effect of the antibody. Bemarituzumab (FUT8-KO) lacks a core fucose in the polysaccharide portion of the Fc domain of the antibody, and results in a high affinity to human FcγRIIIa.

SU11652 is a potent receptor tyrosine kinase (RTK) inhibitor. SU11652 also inhibits several members of the split kinase family of RTKs, including VEGFR, FGFR, PDGFR, and Kit. SU11652 can be uesd for spontaneous cancers expressing Kit mutations research.

Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC₅₀=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC₅₀s=540/800 nM), Lyn (IC₅₀= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity.

BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC₅₀ of 188 nM and a K_d of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces spindle assembly checkpoint (SAC)-dependent mitotic arrest, DNA damage and apoptosis. BO-264 has broad-spectrum antitumor activity.

Ferulic acid sodium is a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor with IC₅₀s of 3.78 and 12.5 μM for FGFR1 and FGFR2, respectively.

Ferulic acid (Standard) is the analytical standard of Ferulic acid. This product is intended for research and analytical applications. Ferulic acid is a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor with IC50s of 3.78 and 12.5 μM for FGFR1 and FGFR2, respectively.

Irpagratinib (ABSK011) is an orally active FGFR4 inhibitor (IC₅₀<10 nM). Irpagratinib inhibits FGFR4 autophosphorylation and blocks signaling from FGFR4 to downstream pathway activation. Irpagratinib has shown high exposure in PK studies in mice, rats, and dogs, and also demonstrated antitumor activity in a subcutaneous xenograft tumor model.

U3-1784 is a humanized antibody expressed in CHO that targets FGFR4/CD334. U3-1784 is equipped with a huIgG1 heavy chain and a huλ light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for U3-1784 can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).

Resigratinib (KIN-3248) is an irreversible and orally active covalent inhibitor of FGFR1-4 that effectively inhibits wild-type and drug-resistant mutations (such as FGFR2 V565F, FGFR3 V555M). Resigratinib covalently binds to the Cys492 site of FGFR, blocks the FGFR signaling pathway, inhibits tumor cell proliferation and induces apoptosis. Resigratinib can be used for the study of FGFR2/3-driven solid tumors (such as cholangiocarcinoma and bladder cancer).

MAX-40279 is a dual and orally active inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 is also effective against the FLT3 mutants such as FLT3^D835Y, suggesting that it can overcome resistance to Quizartinib (HY-13001) and Sorafenib (HY-10201). MAX-40279 inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 can be used for the research of acute myelogenous leukemia (AML).

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.