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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. Aberrant PI3K/Akt is associated with many human cancers. CAY10626 is a potent, dual PI3Kalpha/mTOR inhibitor with IC50 values of 0.9 and 0.6 nM for the two respective kinases. 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. When administered at 25-50 mg/k to MD361 xenograft mice, phosphorylation of the downstream targets of PI3Kalpha and mTOR (Akt T308, Akt S473, and S6K) was suppressed, and significant tumor regression was observed.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: DMF: 15 mg/ml, DMSO: 15 mg/ml, DMSO:PBS (pH 7.2) (1:10): 0.1 mg/ml. lambdamax: 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.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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