A dual PI3Kα/mTOR kinase inhibitor
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CAY10626

Item No. 13838

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-(dimethylamino)ethyl]-N-methyl-4-[[[[4-[4-(4-morpholinyl)-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]phenyl]amino]carbonyl]amino]-benzamide
CAS Number
1202884-94-3
Molecular Formula
C31H35F3N8O3
Formula Weight
624.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMSO: 15 mg/mlDMSO:PBS (pH 7.2) (1:10): 0.1 mg/ml
λmax
289 nm
SMILES
O=C(NC1=CC=C(C(N(C)CCN(C)C)=O)C=C1)NC2=CC=C(C3=NC(N4CCOCC4)=C(C=CN5CC(F)(F)F)C5=N3)C=C2
InChi Code
InChI=1S/C31H35F3N8O3/c1-39(2)14-15-40(3)29(43)22-6-10-24(11-7-22)36-30(44)35-23-8-4-21(5-9-23)26-37-27(41-16-18-45-19-17-41)25-12-13-42(28(25)38-26)20-31(32,33)34/h4-13H,14-20H2,1-3H3,(H2,35,36,44)
InChi Key
GMASZVAHNYVURN-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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    Product Description

    Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3' hydroxyl position of PIs to produce PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3, important second messengers that modulate the activity of downstream targets Akt and mTOR.1 Aberrant PI3K/Akt is associated with many human cancers. CAY10626 is a potent, dual PI3Kα/mTOR inhibitor with IC50 values of 0.9 and 0.6 nM for the two respective kinases.2 In a tumor cell growth inhibition assay, CAY10626 demonstrates IC50 values of <3 and 13 nM for MDA361 (breast) and PC3 (prostate) cancer cell lines, respectively.2 When administered at 25-50 mg/k to MD361 xenograft mice, phosphorylation of the downstream targets of PI3Kα and mTOR (Akt T308, Akt S473, and S6K) was suppressed, and significant tumor regression was observed.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Rameh, L.E., and Cantley, L.C. The role of phosphoinositide 3-kinase lipid products in cell function. The Journal of Biological Chemisty 274(13), 8347-8350 (1999).

    2. Chen, Z., Venkatesan, A.M., Dehnhardt, C.M., et al. Synthesis and SAR of novel 4-morpholinopyrrolopyrimidine derivatives as potent phosphatidylinositol 3-kinase inhibitors. J. Med. Chem. 53(8), 3169-3182 (2010).