WYE-125132
| CAS号 | 1144068-46-1 | 货号 | BCP02227 |
| 中文名 | WYE-125132 | ||
| 英文名 | WYE-125132 | ||
| 中文别名 | |||
| 英文别名 | WYE 125132;WYE125132; | ||
| 分子式 | C26H31N7O4 | 分子量 | 519.61 |
| 生物活性 | WYE-125132 potently and ATP-competitively inhibits recombinant mTOR kinase with IC50 of 0.19 nM and also shows the high selectivity over various PI3Ks and a panel of 230 protein kinases. [1] In vitro, WYE-125132 exhibits a significant anti-proliferative activity against a panel of tumor cell lines with IC50 ranging from 2 nM (LNCap) to 380 nM (HTC116). Besides, WYE-125132 also causes cell cycle progression, induction of apoptosis, and inhibition of protein synthesis and cell size.WYE-125132 results in a significant reduction in the synthesis of pre-tRNALeu by 72%, 80%, and 53% in actively proliferating cells of MG63, MDA361, and HEK293, respectively by inhibiting mTORC1. Moreover, WYE-125132 is also found to induce the dephosphorylation of Maf1 (negative regulator of Pol III transcription) and its accumulation in the nucleus. | ||
| 信号通路 | PI3K/Akt/mTOR | ||
| 靶 点 | mTOR | ||
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mTOR Promotes Tissue Factor Expression and Activity in EGFR-Mutant Cancer
购于瀚香生物(Biochempartner)的WYE-125132(CAS:1144068-46-1)被引用 |
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mTOR complex-2 stimulates acetyl-CoA and de novo lipogenesis through ATP citrate lyase in HER2/PIK3CA-hyperactive breast cancer
购于瀚香生物(Biochempartner)的WYE-125132(CAS:1144068-46-1)被引用 |
结构式
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