BLU9931

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WARNING: This product is for research use only, not for human or veterinary use.

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.

Price and Availability

BLU9931, purity > 98%, is in stock. The same day shipping out after order is received.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 206192Name: BLU9931CAS#: 1538604-68-0Chemical Formula: C26H22Cl2N4O3Exact Mass: 508.1069Molecular Weight: 509.38Elemental 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

Technical Data

Additional Information

References

1: Packer LM, Pollock PM. Paralog-SpecificKinase Inhibition of FGFR4: Adding tothe 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, BifulcoN, 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 ofHepatocellular 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.