BLU9931

SKU: orb1305627

Description

BLU9931

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1538604-68-0
• MW: 509.38
• Purity: 99.85% (May vary between batches)
• Formula: C₂₆H₂₂Cl₂N₄O₃
• SMILES: COc1cc(OC)c(Cl)c(c1Cl)-c1ccc2nc(Nc3c(C)cccc3NC(=O)C=C)ncc2c1
• Target: FGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.96 mM);DMSO:5.1 mg/mL (10.01 mM)

Bioactivity

• Target IC50:
  FGFR2:493 nM|FGFR1:591 nM|FGFR4:3 nM|FGFR3:150 nM
• In Vivo:
  In mice bearing the FGF19-amplified Hep 3B liver tumors, BLU9931 (300 mg/kg, p.o.) leads to tumor regression and prevents this weight loss induced by tumors. In mice bearing the FGF19-overexpressing PDX-derived LIXC012 xenografts, treatment with BLU9931 (300 mg/kg, p.o.) also leads to tumor regression.
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• 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.
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• Cell Research:
  Established and PDX-derived HCC cell lines are seeded in 96-well plates in respective growth media, allowed to attach overnight, and treated with a dilution series of test compounds for two cell-doubling times. Cell viability is determined by CellTiter-Glo, and results represented as background-subtracted relative light units normalized to a DMSO-treated control. Relative EC50 values are determined at 50% inhibition between the top and bottom plateau of the dose–response curve.(Only for Reference)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Fibroblast growth factor receptor, FGFR1, FGFR, FGFR2, FGFR3, FGFR4, Inhibitor, BLU 9931, BLU9931, BLU-9931

Compound Identifiers

PubChem CID

72710839