AZD8055
| CAS号 | 1009298-09-2 | 货号 | BCP02171 |
| 中文名 | AZD8055 | ||
| 英文名 | AZD8055 | ||
| 中文别名 | |||
| 英文别名 | AZD-8055;AZD 8055;CCG-168;CCG168;CCG 168; | ||
| 分子式 | C25H31N5O4 | 分子量 | 465.56 |
| 生物活性 | AZD8055 shows low activity (～1,000-fold) against all PI3K isoforms (α, β, γ, δ) and other members of the PI3K-like kinase family (ATM and DNA-PK). AZD8055 inhibits the phosphorylation of mTORC1 (p70S6K and 4E-BP1) as well as phosphorylation of the mTORC2 (Akt) and downstream proteins. The rapamycin-resistant T37/46 phosphorylation sites on 4E-BP1 can be fully inhibited by AZD8055, resulting in significant inhibition of cap-dependent translation. AZD8055 potently inhibits proliferation in U87MG, A549 and H838 cells with IC50 of 53, 50 and 20 nM, respectively. AZD8055 also induces autophagy and increased LC3-II levels in H838 and A549 cells.AZD8055 decreases AML blast cell proliferation and cell cycle progression, reduces the clonogenic growth of leukemic progenitors and induces caspase-dependent apoptosis in leukemic cells but not in normal immature CD34+ cells. AZD8055 indicates inhibitory against the pediatric preclinical testing program (PPTP) cell lines with IC50 of 24.7?nM and indu | ||
| 信号通路 | PI3K/Akt/mTOR | ||
| 靶 点 | mTOR | ||
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A novel lead compound CM-118: Antitumor activity and new insight into the molecular mechanism and combination therapy strategy in c-Met- and ALK-dependent cancers
购于瀚香生物(Biochempartner)的AZD8055(CAS:1009298-09-2)被引用 |
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Molecular regulation of apoptotic machinery and lipid metabolism by mTORC1/mTORC2 dual inhibitors in preclinical models of HER2+/PIK3CAmut breast cancer
购于瀚香生物(Biochempartner)的AZD8055(CAS:1009298-09-2)被引用 |
结构式
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