货号 | 4823/10 |
别名 | N-[4-[[4-(Dimethylamino)-1-piperidi |
供应商 | Tocris |
生物活性 | Potent and selective dual inhibitor of PI 3-kinase/mTOR (IC50 values are 0.4, 1.6 and 5.4 nM for PI 3-Kα, mTOR and PI 3-Kγ respectively). Exhibits selectivity over 234 other protein kinases (IC50>10μM). Potently inhibits tumor cell growth in 37 different tumor cell lines (IC50 < 100 nM). Also exhibits antitumor activity in MDA-361, HCT-116, H1975 and U87MG xenograft models. |
运输条件 | Blue Ice |
存放说明 | -20℃ |
纯度 | >98 % |
计算分子量 | 615.73 |
分子式 | C32H41N9O4 |
可溶性/溶解性 | Soluble to 5 mM in DMSO with gentle warming |
参考文献 | Mallonet al (2011) Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor. Clin.Cancer Res. 17 3193. PMID: 21325073. Venkatesanet al (2010) Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor. J.Med.Chem. 53 2636. PMID: 20166697. |