BLU 9931
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- Product name: BLU 9931
- CAS: 1538604-68-0
- MF: C26H22Cl2N4O3
- MW: 509.38
- EINECS:-0
- MDL Number:MFCD28900729
- Synonyms:BLU 9931;BLU9931;BLU-9931;LM-3610;LM-3610; BLU9931;N-(2-((6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)amino)-3-methylphenyl)acrylamide;N-[2-[[6-(2,6-Dichloro-3,5-dimethoxyphenyl)-2-quinazolinyl]amino]-3-methylphenyl]-2-propenamide;2-Propenamide,N-[2-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-quinazolinyl]amino]-3-methylphenyl]-
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Properties
Density :1.361±0.06 g/cm3(Predicted)
storage temp. :Store at -20°C
solubility :≥50.9 mg/mL in DMSO; insoluble in H2O; ≥2.53 mg/mL in EtOH with gentle warming and ultrasonic
form :Powder
pka :13.15±0.70(Predicted)
color :Off-white to light yellow
storage temp. :Store at -20°C
solubility :≥50.9 mg/mL in DMSO; insoluble in H2O; ≥2.53 mg/mL in EtOH with gentle warming and ultrasonic
form :Powder
pka :13.15±0.70(Predicted)
color :Off-white to light yellow
Safety Information
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Description
Fibroblast growth factor receptor 4 (FGFR4) is the receptor for fibroblast growth factor 19 (FGF19), which is a tightly controlled hormone that regulates bile acid synthesis and hepatocyte proliferation in the normal liver. Aberrant signaling through the FGFR4/FGF19 signaling complex has been implicated in hepatocellular carcinoma (HCC). BLU9931 is a small molecule inhibitor of FGFR4 (IC50 = 3 nM) that is selective for FGFR4 over other FGFR family members (IC50s = 591, 493, and 150 nM for FGFR1, 2, and 3, respectively) and an extensive panel of additional kinases (selectivity score for BLU9931 at 3 μM is 0.005). It inhibits proliferation of HCC cell lines with an activated FGFR4 signaling pathway (EC50s = 0.02-0.11 μM) and demonstrates antitumor activity when administered orally at 100 mg/kg to mice bearing HCC xenografts that overexpresses FGF19 due to amplification or to mice bearing liver tumor xenografts that overexpresses FGF19 mRNA but lack FGF19 amplification.More related product prices
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