For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>BLU9931 is the first selective small molecule inhibitor of FGFR4 with IC50 of 3 nM; less potent for FGFR1/2/3(IC50> 150 nM).<br>IC50 value:<br>Target: FGFR4 selective inhibitor<br>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.</p>
Catalog Number | I001936 |
CAS Number | 1538604-68-0 |
Synonyms | N-(2-((6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)amino)-3-methylphenyl)acrylamide |
Molecular Formula | C₂₆H₂₂Cl₂N₄O₃ |
Purity | ≥95% |
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 |
Reference | <p style=/line-height:25px/> |