FGFR2 Inhibitor

HuGAL-FR21 is a humanized antiFGFR2IIIb IgG1 monoclonal antibody. HuGAL-FR21 can block the binding of FGF2, FGF7, and FGF10 to FGFR2IIIb and inhibit FGF-induced phosphorylation of FGFR2IIIb. HuGAL-FR21 can downregulate the expression of FGFR2 in SNU-16 cells. HuGAL-FR21 shows the significant anti-tumor activity in athymic nude mice bearing gastric cancer xenograft models. HuGAL-FR21 can be used for research on cancer such as gastric cancer.

Lavengratinib (ABSK061) is a FGFR2/FGFR3 inhibitor. Lavengratinib selectively inhibits FGFR2 and FGFR3 signaling pathways and reduces the risk of FGFR1-mediated hyperphosphatemia. Lavengratinib is suitable for research on advanced solid tumors (including cholangiocarcinoma, gastric cancer, non-small cell lung cancer, cervical cancer and urothelial cancer).

FGFR-IN-27 is an orally active, broad-spectrum FGFR inhibitor, with an IC₅₀ of 0.24 nM against human FGFR1, 0.71 nM against FGFR2, 0.87 nM against FGFR3, and 6.50 nM against FGFR4. FGFR-IN-27 inhibits cancer cell proliferation and blocks tumor growth. FGFR-IN-27 reduces the phosphorylation levels of AKT and ERK, induces apoptosis and ferroptosis, increases ROS levels, and decreases GSH levels. FGFR-IN-27 can be used in the research of hepatocellular carcinoma.

FGFR-IN-28 is a FGFR inhibitor with inhibitory activity against multiple subtypes of the FGFR family, with an IC₅₀ of 4.4 nM against FGFR4. FGFR-IN-28 inhibits kinase activity and phosphorylation processes, and blocks the downstream MAPK and AKT signaling pathways. FGFR-IN-28 induces cellular DNA damage, cell cycle arrest, apoptosis and ferroptosis, and reduces the adhesion, invasion and metastasis abilities of cancer cells. FGFR-IN-28 exhibits anti-tumor activity in in vitro experiments on colon cancer cells, and inhibits tumor growth in colon cancer xenograft models. FGFR-IN-28 can be used in colon cancer-related research.

FGFR-IN-29 is an orally active pan-FGFR inhibitor that suppresses the kinase activities of FGFR1, FGFR2, FGFR3, and FGFR4. FGFR-IN-29 blocks the intracellular phosphorylation process of FGFR and arrests downstream tumor cell proliferation signaling. FGFR-IN-29 inhibits tumor growth in solid tumor xenograft mouse models. FGFR-IN-29 is applicable for cancer-related research.

PD173074 GMP is PD173074 (HY-10321) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. PD173074 is an orally active FGFR inhibitor that targets the transphosphorylation of FGFR1 and FGFR2 and blocks the FGF signaling pathway. By reducing the phosphorylation level of SMAD2 and altering the expression of Nodal/Activin target genes, PD173074 eliminates endothelial differentiation potential, thereby inhibiting the formation of capillary-like structures. PD173074 blocks the proliferation and colony formation of tumor cells and increases intratumoral cell apoptosis. PD173074 successfully reverses FGF-2-induced chemoresistance to enhance the effect of cisplatin (HY-17394) in small cell lung cancer models. PD173074 can be applied to research related to critical limb ischemia and small cell lung cancer.

FGFR3-IN-12 is a selective fibroblast growth factor receptor 3 (FGFR3) inhibitor with an IC₅₀ of 6.8 nM. FGFR3-IN-12 shows an IC₅₀ of 19.2 nM against FGFR3^V555M and an IC₅₀ of 16.9 nM against TNK1 (Thirty-eight Negative Kinase 1). FGFR3-IN-12 inhibits cancer cells proliferation and induces caspase-mediated apoptosis. FGFR3-IN-12 exhibits antitumor activity in bladder cancer xenografts mice models. FGFR3-IN-12 can be used for the research of cancer, such as bladder cancer.

FGFR-IN-12 (example 14), a pyrimidinyl aryl urea derivative, is a potent FGFR inhibitor.

FGFR2-IN-4 is a selective, orally active FGFR2 inhibitor, with IC₅₀ values of 10.0 nM and 5.8 nM against wild-type FGFR2 and the FGFR2^V565F mutant, respectively. FGFR2-IN-4 induces necroptosis in FGFR2-driven tumor cells. FGFR2-IN-4 induces tumor regression in xenograft models harboring FGFR2 inhibitor-resistant mutations without altering serum phosphate levels. FGFR2-IN-4 is used to investigate FGFR2-driven malignancies, including intrahepatic cholangiocarcinoma and gastric cancer.

GP369 is a humanized FGFR2-IIIb-specific antibody. GP369 significantly inhibits the proliferation of tumor cells. GP369 can significantly inhibit phosphorylation of FGFR2 and downstream signaling pathways. GP369 can be used for research on cancer such as gastric cancer and breast cancer.