MTI-31
| CAS号 | 1567915-38-1 | 货号 | BCP36715 |
| 中文名 | MTI-31 | ||
| 英文名 | MTI-31 | ||
| 中文别名 | |||
| 英文别名 | MTI31;MTI 31;LXI-15029;mTOR inhibitor-31; | ||
| 分子式 | C26H30N6O3 | 分子量 | 474.57 |
| 生物活性 | MTI-31 is a novel potent, selective mTORC1/mTORC2 inhibitor with Kd of 0.2 nM (mTOR), displays >5,000-fold selectivity over PIK3CA, PIK3CB and PIK3G; showed an IC50 value 39 nM in LANCE® assay of mTOR substrate phosphorylation; dose-dependently inhibits of both the mTORC1 substrates P-S6K1(T389), P-S6(S235/6), P-4EBP1(T70) and mTORC2 substrate P-AKT(S473) tumor cell lines harboring mTOR pathway dysregulation with IC50 of <0.12 uM; potently inhibited cell proliferation (IC50 <1 mmol/L) and in vivo tumor growth in multiple NSCLC models of EGFR/T790M, EML4-ALK, c-Met or KRAS (MED <10 mg/kg), also suppressed programmed death ligand 1 (PD-L1) in EGFR- and ALK-driven NSCLC, mediated in part by mTORC2/AKT/GSK3β-dependent proteasomal degradation. | ||
| 信号通路 | PI3K/Akt/mTOR | ||
| 靶 点 | mTOR | ||
结构式
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