BLU9931

• CAT Number: I001936
• CAS Number: 1538604-68-0
• Molecular Formula: C₂₆H₂₂Cl₂N₄O₃
• Molecular Weight: 509.38
• Purity: ≥95%
• Synonyms: N-(2-((6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)amino)-3-methylphenyl)acrylamide
• Target: FGFR
• Solubility: DMSO: ≥ 17 mg/mL
• Storage: Store at -20°C
• InChI: InChI=1S/C26H22Cl2N4O3/c1-5-21(33)30-18-8-6-7-14(2)25(18)32-26-29-13-16-11-15(9-10-17(16)31-26)22-23(27)19(34-3)12-20(35-4)24(22)28/h5-13H,1H2,2-4H3,(H,30,33)(H,29,31,32)
• InChIKey: TXEBNKKOLVBTFK-UHFFFAOYSA-N
• SMILES: CC1=C(C(=CC=C1)NC(=O)C=C)NC2=NC=C3C=C(C=CC3=N2)C4=C(C(=CC(=C4Cl)OC)OC)Cl

BLU9931 (Cat  No.: I001936) is a potent, selective, and irreversible inhibitor of fibroblast growth factor receptor 4 (FGFR4), with high specificity over other FGFR isoforms. It covalently binds to a unique cysteine residue in FGFR4, effectively blocking its kinase activity. BLU9931 is primarily used in cancer research, particularly in studies involving hepatocellular carcinoma (HCC), where FGFR4 signaling is implicated in tumor progression. Its high selectivity and strong inhibitory activity make it a valuable tool for exploring FGFR4-targeted therapies and understanding related signaling pathways.

Reference

[1]. Hagel M, et al. First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway. Cancer Discov. 2015 Apr;5(4):424-37.
[2]. Packer LM, et al. Paralog-Specific Kinase Inhibition of FGFR4: Adding to the Arsenal of Anti-FGFR Agents. Cancer Discov. 2015 Apr;5(4):355-7.