FGFR3 Inhibitor

IMC-D11 (LY-3076226 antibody) is an anti-FGFR3 IgG1 monoclonal antibody with an EC₅₀ of approximately 0.1 nM against hFGFR3b and hFGFR3c. IMC-D11 inhibits the growth of FGFR3-dependent lung adenocarcinoma in mouse models and shows no effect on tumors that do not express FGFR3. IMC-D11 can serve as an ADC Antibody for ADC synthesis, such as LY3076226. IMC-D11 is applicable to research related to urothelial carcinoma, multiple myeloma, lung adenocarcinoma, as well as advanced or metastatic cancers.

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).

FGFR3-IN-10 is a FGFR3 inhibitor with an IC₅₀ of <350 nM. FGFR3-IN-10 is applicable to research related to cancer, systemic sclerosis, fibrosis, achondroplasia, thanatophoric dysplasia, and Muenke syndrome.

Dabogratinib (GMP) is the GMP-grade version of Dabogratinib (HY-159642). Dabogratinib (TYRA-300) is an orally active, selective FGFR3 inhibitor with an IC₅₀ of 11 nM. Dabogratinib exhibits antitumor activity against urothelial carcinoma and solid tumors. Dabogratinib downregulates the FGFR3 and ERK1/2 signaling pathways, and induces tumor growth inhibition and regression in FGFR3-altered xenograft models. Dabogratinib promotes chondrocyte proliferation and differentiation, drives endochondral bone formation and overall body growth, partially restores long bone proportions, and improves craniofacial and spinal morphology. Dabogratinib can be used for the research of metastatic urothelial carcinoma, achondroplasia and hypochondroplasia.

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.

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.

FGFR3-IN-11 (compound B10) is a Fibroblast growth factor receptor 3 (FGFR3) inhibitor with a K_a value of 4.8 μM. FGFR3-IN-11 induces apoptosis, suppresses colony formation, and causes dose-dependent G0/G1 cell cycle arrest in cancer cells. FGFR3-IN-11 exerts anticancer activity against cancer cells with minimal toxicity toward normal hepatocytes and demonstrates tumor growth suppression in xenograft mouse models. FGFR3-IN-11 can be used for the research of hepatocellular carcinoma.