An inhibitor of FGFR1, 2, and 3
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CH5183284

Item No. 17120

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
[5-amino-1-(2-methyl-1H-benzimidazol-6-yl)-1H-pyrazol-4-yl]-1H-indol-2-yl-methanone
CAS Number
1265229-25-1
Synonyms
  • Debio 1347
Molecular Formula
C20H16N6O
Formula Weight
356.4
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlDMSO:PBS (pH 7.2) (1:6): 0.1 mg/mlEthanol: 1 mg/ml
λmax
212, 342 nm
SMILES
NC1=C(C(C2=CC3=C(C=CC=C3)N2)=O)C=NN1C4=CC(NC(C)=N5)=C5C=C4
InChi Code
InChI=1S/C20H16N6O/c1-11-23-16-7-6-13(9-17(16)24-11)26-20(21)14(10-22-26)19(27)18-8-12-4-2-3-5-15(12)25-18/h2-10,25H,21H2,1H3,(H,23,24)
InChi Key
BEMNJULZEQTDJY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

    $238

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    25 mg

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    Product Description

    CH5183284 is a potent, selective inhibitor of the kinase activity of fibroblast growth factor receptors (FGFRs) 1, 2, and 3 (IC50s = 9.3, 7.6, and 22 nM, respectively).1 It less potently inhibits FGFR4 and platelet-derived growth factor receptor β (IC50s = 290 and 560 nM, respectively) and displays IC50 values greater than 1 µM for a diverse panel of tyrosine and serine/threonine kinases.1 CH5183284 is effective against FGFR2 containing the gatekeeper mutation V564F.1 Moreover, it inhibits the growth of cancer cells expressing FGFR genetic alterations both in vitro and in xenograft mouse models.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Nakanishi, Y., Akiyama, N., Tsukaguchi, T., et al. The fibroblast growth factor receptor genetic status as a potential predictor of the sensitivity to CH5183284/Debio 1347, a novel selective FGFR inhibitor. Mol. Cancer Ther. 13(11), 2547-2558 (2014).