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. Aberrent 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.In a tumor cell growth inhibition assay, CAY10626 demonstrates IC₅₀ values of <3 and 13 nm for mda361 (breast) pc3 (prostate) cancer cell lines, respectively. when administered at 25-50 mg>

Store at -20° C

Solid

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

~1.4 g/cm³ (Predicted)

~646.1 °C at 760 mmHg (Predicted)

n²⁰_D 1.63 (Predicted)

mTOR: IC₅₀ = 0.6 nM (human); PI3Kα: IC₅₀ = 0.9 nM (human); MDA361: IC₅₀ = <3 nm (human); pc3: ic₅₀ = <13 nM (human)

pK_a: 13.75 (Predicted), pK_b: 8.38 (Predicted)

Soluble in DMSO (~15 mg/ml), DMF (~15 mg/ml), and 1:10DMSO:PBS(pH7.2) (~0.1 mg/ml).

MFCD18251469

44599690