A multi-targeted kinase inhibitor
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CAY10717

Item No. 19955

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[[[2-methyl-5-[[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)benzoyl]amino]phenyl]methyl]amino]-1H-pyrrolo[2,3-b]pyridine-2-carboxylic acid, methyl ester
CAS Number
1240322-54-6
Molecular Formula
C29H25F3N6O3
Formula Weight
562.5
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS(pH7.2) (1:2): 0.33 mg/mlDMSO: 12.5 mg/mlEthanol: 0.5 mg/ml
λmax
234, 299, 378 nm
SMILES
O=C(OC)C1=CC2=CC(NCC3=C(C)C=CC(NC(C4=CC(N5C=NC(C)=C5)=CC(C(F)(F)F)=C4)=O)=C3)=CN=C2N1
InChi Code
InChI=1S/C29H25F3N6O3/c1-16-4-5-22(8-20(16)12-33-23-7-18-10-25(28(40)41-3)37-26(18)34-13-23)36-27(39)19-6-21(29(30,31)32)11-24(9-19)38-14-17(2)35-15-38/h4-11,13-15,33H,12H2,1-3H3,(H,34,37)(H,36,39)
InChi Key
PGQWALGGBUYLQF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    CAY10717 is a multi-targeted kinase inhibitor that exhibits greater than 40% inhibition of 34 of 104 kinases in an enzymatic assay at a concentration of 100 nM.1 It has activity at multiple oncogenic kinases, with IC50 values less than 50 nM against wild-type EGFR and ABL and mutant ABLG250E, ABLY253F, ABLE255K, and B-RafV600E. CAY10717 is highly cytotoxic against a cancer cell panel that includes chemotherapy-sensitive and -resistant cell lines (EC50s = 0.4-158 nM). It also inhibits the growth of human umbilical vein endothelial cells (HUVECs; EC50 = 34 nM), a model for tumor angiogenesis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Daydé-Cazals, B., Fauvel, B., Singer, M., et al. Rational design, synthesis, and biological evaluation of 7-azaindole derivatives as potent focused multi-targeted kinase inhibitors. J. Med. Chem. 59(8), 3886-3905 (2016).