WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206192
Description: BLU9931 is a potent and irreversible small-molecule inhibitor of FGFR4, as a targeted therapy to treat patients with HCC whose tumors have an activated FGFR4 signaling pathway. BLU9931 is exquisitely selective for FGFR4 versus other FGFR family members and all other kinases. BLU9931 shows remarkable antitumor activity in mice bearing an HCC tumor xenograft that overexpresses FGF19 due to amplification as well as a liver tumor xenograft that overexpresses FGF19 mRNA but lacks FGF19 amplification. Approximately one third of patients with HCC whose tumors express FGF19 together with FGFR4 and its coreceptor klotho β (KLB) could potentially respond to treatment with an FGFR4 inhibitor.
MedKoo Cat#: 206192
Chemical Formula: C26H22Cl2N4O3
Exact Mass: 508.1069
Molecular Weight: 509.38
Elemental Analysis: C, 61.31; H, 4.35; Cl, 13.92; N, 11.00; O, 9.42
Synonym: BLU9931; BLU-9931; BLU 9931.
IUPAC/Chemical Name: N-(2-((6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)amino)-3-methylphenyl)acrylamide
InChi Key: TXEBNKKOLVBTFK-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: C=CC(NC1=CC=CC(C)=C1NC2=NC=C3C=C(C4=C(Cl)C(OC)=CC(OC)=C4Cl)C=CC3=N2)=O
1: Packer LM, Pollock PM. Paralog-Specific Kinase Inhibition of FGFR4: Adding to the Arsenal of Anti-FGFR Agents. Cancer Discov. 2015 Apr;5(4):355-7. doi: 10.1158/2159-8290.CD-15-0246. PubMed PMID: 25847957.
2: Hagel M, Miduturu C, Sheets M, Rubin N, Weng W, Stransky N, Bifulco N, Kim JL, Hodous B, Brooijmans N, Shutes A, Winter C, Lengauer C, Kohl NE, Guzi T. 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. doi: 10.1158/2159-8290.CD-14-1029. Epub 2015 Mar 16. PubMed PMID: 25776529.