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BLU9931 is a potent, selective, and irreversible FGFR4 inhibitor with an IC50 of 3 nM and 297,184, and 50-fold higher selectivity than FGFR1/2/3, respectively.
Brand: BCM
Target: FGFR
Signaling Pathways: Angiogenesis; Tyrosine Kinase/Adaptors
In Vitro: In MDA-MB-453 cells, BLU9931 potently inhibits phosphorylation of FGFR4 signaling pathway. BLU9931 inhibits proliferation of HCC cell lines that express an intact FGFR4 signaling complex, such as Hep 3B, HUH-7, and JHH-7 cell lines, with EC50 of <1 μM. BLU9931 also inhibits proliferation in PDX-derived cell lines with an intact FGFR4 signaling pathway.
pKa: 13.15±0.70(Predicted)
Solubility: Soluble in DMSO. Insoluble in Water; Insoluble in Ethanol.
GHS: GHS07
Isomeric 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
InChIKey: TXEBNKKOLVBTFK-UHFFFAOYSA-N
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)
Attribute [CAS No.] 1538604-68-0 [Formula] C26H22Cl2N4O3 [Molecular] 509.38 [Chem Name] N-[2-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl]amino]-3-methylphenyl]prop-2-enamide [Synonym] BLU9931 [Storage] Keep in dark place. Sealed in dry, 2-8°C [MDL No.] MFCD28900729 [Form] Powder
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