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BLU-9931

Cat. No. M5253

BLU-9931 Structure

Synonym: BLU9931

Size Price Availability Quantity
5mg USD 120 In stock
10mg USD 180 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

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.

Protocol
Cell Experiment
Cell lines Hep 3B, HUH-7, JHH-7, PLC/PRF/5, SK-HEP-1, SNU-182, SNU-387, SNU-398, SNU-423, SNU-449, SNU-878 cells
Preparation method 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.
Concentrations ~10 μM
Incubation time 72-120 hours
Animal Experiment
Animal models Mice bearing LIXC012 tumors
Formulation 0.5% carboxymethylcellulose/1% Tween 80 as a suspension
Dosages ~300 mg/kg
Administration p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 509.38
Formula C26H22Cl2N4O3
CAS Number 1538604-68-0
Purity >99%
Solubility 4 mg/mL warmed in DMSO
Storage at -20°C
References

Paralog-Specific Kinase Inhibition of FGFR4: Adding to the Arsenal of Anti-FGFR Agents.
Packer LM, et al. Cancer Discov. 2015 Apr;5(4):355-7. PMID: 25847957.

First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway.
Hagel M, et al. Cancer Discov. 2015 Apr;5(4):424-37. PMID: 25776529.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BLU-9931, BLU9931 supplier, FGFR, inhibitors

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