CAY10626 是一种 PI3Kα/mTOR 双激酶抑制剂。 CAY10626 的 IC50 为 0.9,PI3Kα 的 IC50 为 0.6 nM;和 mTOR,分别。 CAY10626可用于癌症的研究。
Cas No. | 1202884-94-3 |
化学名 | 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 |
Canonical 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 |
分子式 | C31H35F3N8O3 |
分子量 | 624.7 |
溶解度 | DMF: 15 mg/ml,DMSO: 15 mg/ml,DMSO:PBS (pH 7.2) (1:10): 0.1 mg/ml |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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 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 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. |