FGFR Inhibitor

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.

Rogaratinib (BAY1163877) is a potent and selective fibroblast growth factor receptor (FGFR) inhibitor. Rogaratinib inhibits FGFRs with IC50s of 11.2 nM (FGFR1), <1 nM (FGFR2), 18.5 nM (FGFR3), 127 nM (VEGFR3/FLT4), 201 nM (FGFR4), respectively.

LY2874455 is a pan-FGFR inhibitor with IC₅₀s of 2.8, 2.6, 6.4, 6 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively.

Vofatamab (B-701) is an anti-FGFR3 monoclonal antibody (mAb). Vofatamab blocks activation of both the wildtype and genetically activated receptor. Vofatamab can be used in the research of metastatic urothelial carcinoma (mUC). Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).

Infigratinib phosphate (BGJ-398 phosphate; NVP-BGJ398 phosphate) is a potent inhibitor of the FGFR family with IC₅₀ of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.

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.

β,β-Dimethylacrylalkannin (Arnebin 1) is an orally active FGFR1 inhibitor (IC₅₀=2.5 μM) and the main active component of Lithospermum erythrorhizon. β,β-Dimethylacrylalkannin blocks downstream signaling by binding to the ATP pocket of FGFR1, and regulates the CDK1/Cdc25C pathway and ROS-JNK axis, thereby inducing G2/M phase arrest, necrosis and apoptosis in cancer cells, and inhibiting tumor proliferation. β,β-Dimethylacrylalkannin also acts as a colistin adjuvant to disrupt the cell membrane of Gram-negative bacteria. β,β-Dimethylacrylalkannin exhibits significant tumor-inhibitory effects with no obvious toxicity in PDX models, but chronic exposure to high doses may alter the relative lung/liver weights of rats, while acute exposure to high doses causes responses such as reduced motor activity. β,β-Dimethylacrylalkannin finds wide application in studies related to hepatocellular carcinoma, colorectal cancer, colistin-resistant bacterial infections, hepatitis and psoriasis.

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.

ENMD-2076 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, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.

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.

Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). Anticancer and antiangiogenic activity.

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.

Tinengotinib (TT00420) is an orally active, spectrally selective small molecule kinase inhibitor targeting Aurora A/B (IC₅₀=1.2-3.3 nM), FGFR1/2/3 (IC₅₀=1.5-3.5 nM), VEGFRs, JAK1/2 and CSF1R. Tinengotinib blocks Aurora kinase-mediated cell cycle progression (inducing G2/M arrest), inhibits FGFR/JNK-JUN signaling pathway and activates MEK/ERK-dependent apoptotic pathway. Tinengotinib has the activity of anti-tumor proliferation, inducing apoptosis, inhibiting angiogenesis and regulating tumor microenvironment. Tinengotinib can be used in the study of triple-negative breast cancer (TNBC), gallbladder cancer and tumor immune microenvironment.

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.

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.

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.

Lucitanib (E-3810) is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC₅₀s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.

FIIN-2 is an irreversible inhibitor of FGFR with an IC₅₀ of 3.1, 4.3, 27, and 45 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.