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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

CAY10626 Exclusive

Cayman Chemical Item Number 13838

(CAS 1202884-94-3)

CAY10626 (CAS 1202884-94-3)

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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

1 Rameh, L.E., and Cantley, L.C. The role of phosphoinositide 3-kinase lipid products in cell function. J Biol Chem 274 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).

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
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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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

Background Reading

Rameh, L.E., and Cantley, L.C. The role of phosphoinositide 3-kinase lipid products in cell function. J Biol Chem 274 8347-8350 (1999).

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).
Size Price Quantity Subtotal
1 mg $84.00 $0.00
5 mg $378.00 $0.00
10 mg $672.00 $0.00
25 mg $1,470.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

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Pricing updated 2012-02-11. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

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