A selective FGFR4 inhibitor
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BLU-9931

Item No. 18405

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-quinazolinyl]amino]-3-methylphenyl]-2-propenamide
CAS Number
1538604-68-0
Molecular Formula
C26H22Cl2N4O3
Formula Weight
509.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS(pH 7.2) (1:2): 0.3 mg/mlEthanol: 0.2 mg/ml
λmax
251 nm
SMILES
ClC1=C(C2=CC(C=NC(NC3=C(C)C=CC=C3NC(C=C)=O)=N4)=C4C=C2)C(Cl)=C(OC)C=C1OC
InChi Code
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)
InChi Key
TXEBNKKOLVBTFK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $54

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    5 mg

    $238

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    10 mg

    $418

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    25 mg

    $783

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    Product Description

    BLU-9931 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 BLU-9931 at 3 µM is 0.005).1 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.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hagel, M., Miduturu, C., Sheets, M., et al. First selective small molecule inhibitor of FGFR4 for the treatment of hepatocellular carcinomas with an activated FGFR4 signaling pathway. Cancer Discov. 5(4), 424-437 (2015).