PKI-179 (hydrochloride) 是一种有效且具有口服活性的双重 PI3K/mTOR 抑制剂，对 PI3K-α、PI3K-β、PI3K-γ、PI3K 的 IC50 分别为 8 nM、24 nM、74 nM、77 nM 和 0.42 nM -δ 和 mTOR，分别。 PKI-179 (hydrochloride) 也表现出对 E545K 和 H1047R 的活性，IC50 分别为 14 nM 和 11 nM。 PKI-179（盐酸盐）在体内显示出抗肿瘤活性。
| Cas No. | 1463510-35-1 |
| Canonical SMILES | O=C(NC1=CC=C(C2=NC(N3CCOCC3)=NC(N4C5COCC4CC5)=N2)C=C1)NC6=CC=NC=C6.Cl |
| 分子式 | C25H28N8O3•HCl |
| 分子量 | 525 |
| 溶解度 | DMF: 2 mg/ml,DMSO: 2.5 mg/ml,DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml,Ethanol: slightly soluble |
| 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 | PKI-179 is an orally bioavailable dual inhibitor of PI3K and mammalian target of rapamycin (mTOR). In an in vitro enzymatic assay, it potently inhibits PI3K (IC50s = 8, 24, 17, and 74 nM for isoforms α, β, δ, and γ, respectively), two common PI3Kα mutants, E545K and H1047R (IC50s = 14 and 11 nM, respectively), and mTOR (IC50 = 0.42 nM). PKI-179 is selective for PI3K and mTOR over a panel of 361 other kinases at IC50 values up to 50 μM, hERG (IC50 >30 μM), and cytochrome P450 (CYP) isoforms (IC50s >30 μM), but does have activity for CYP2C8 (IC50 = 3 μM). It inhibits proliferation through the Akt/mTOR signaling pathway in MDA-361 breast and PC3MM2 prostate cancer cell lines in vitro (IC50s = 22 and 29 nM, respectively) and inhibits tumor growth in an MDA-361 mouse xenograft model when used at a dose of 50 mg/kg. |
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