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抑制剂/激活剂

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凋亡与自噬

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AZD8055

AZD8055是一种新型的，ATP竞争性mTOR抑制剂，在MDA-MB-468 细胞中IC50为0.8 nM，与作用于PI3K亚型和ATM/DNA-PK相比，具有优异的选择性（约1000倍）。AZD8055可诱导半胱天冬酶依赖的凋亡和自噬。Phase 1。

货号：
TK0414
规格：

1mg

5mg

10mg

50mg
价格：
￥0.00

产品参数

CAS No.	1009298-09-2
生物活性	AZD-8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM. AZD-8055 inhibits both mTORC1 and mTORC2.
分子式	C25H31N5O4
分子量	465.54
储存条件	Powder -20℃ 3 years
溶解性数据	DMSO : 200 mg/mL (429.61 mM; Need ultrasonic)
体内研究	In mice bearing U87-MG (PTEN null) glioblastoma xenografts, oral treatment with AZD-8055 (AZD8055) results in a dose-dependent tumor growth inhibition of 33%, 48%, and 77% with 2.5, 5, and 10 mg/kg/d twice daily, respectively. A similar dose dependency is observed in nude mice bearing A549 xenografts: tumor growth inhibition is 44%, 55%, and 93% after 2.5, 5, and 10 mg/kg/d twice daily, respectively. AZD8055 also results in significant inhibition of tumor growth and/or regression in breast, lung, colon, prostate, and uterine xenograft models when administered either twice daily at 10 mg/kg or daily at a dose of 20 mg/kg. AZD8055 markedly decreases the phosphorylation levels of mTOR and its substrates and the activation of microglia in vivo, and promotes the microglial polarization from M1 phenotype to M2 phenotype. In addition, administration of AZD8055 following subarachnoid hemorrhage (SAH) significantly ameliorates EBI, including neuronal apoptosis, neuronal necrosis, brain edema and blood-brain barrier permeability.
体外研究	The inhibitory activity of AZD-8055 (AZD8055) against mTOR is evaluated using two different assays. Using the truncated recombinant mTOR enzyme, the IC50 for AZD8055 is 0.13±0.05 nM. Using native mTOR enzyme complexes extracted from HeLa cells, the IC50 is 0.8±0.2 nM. AZD-8055 shows excellent selectivity (~1,000-fold) against all class I PI3K isoforms and other members of the PI3K-like kinase family. AZD-8055 inhibits the phosphorylation of mTORC1 substrates p70S6K and 4E-BP1 as well as phosphorylation of the mTORC2 substrate AKT and downstream proteins. The cellular IC50s for AZD8055 are calculated as 24±9 nM (n=13) for pAKT Ser and 27±3 nM (n=12) for pS6 Ser in MDA-MB-468 cells.
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纯度及产品资料	98%

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