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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; | ||
SMILES | CC1COCCN1C2=NC3=C(C=CC(=N3)C4=CC(=CC=C4)C(=O)NC)C(=N2)N5C6CCC5COC6 | ||
化学名称 | |||
分子式 | C26H30N6O3 | 分子量 | 474.57 |
纯度 | 98% | 配送 | 惯例下常温包邮 |
产品描述 | 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. |
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