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Products are for research use only. Not for human use. We do not sell to patients.
(AZD8055; AZD 8055)
AZD-8055 Chemical Structure
|Product name: AZD-8055|
|Cat. No.: HY-10422|
AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM with excellent selectivity (～1,000-fold) against PI3K isoforms and ATM/DNA-PK.
IC50 value: 0.8 nM 
in vitro: 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 .
in vivo: AZD8055 inhibits the pS6 and pAkt in U87MG and A549 xenografts at 2.5/10 mg/kg, which leads to tumor growth inhibition. AZD8055 shows significant antitumor activity in many xenografts, including U87MG, BT474c, A549, Calu-3, LoVo, SW620, PC3 and MES-SA at a dose of 10/20 mg/kg . AZD8055 induces ~40% reduction in tumour volume, accompanied by ablation of phosphorylation of Akt, S6K and SGK protein kinases. Administration of AZD8055 (5mg/kg, Bid) and SAHA (100 mg/kg/d) results in complete tumor growth inhibition in PTEN+/?LKB1+/hypo xenografts without side effects on mice by inhibition of mTORC1 and mTORC2 signaling .
|M.Wt||465.54||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||2.1480 mL||10.7402 mL||21.4804 mL|
|5 mM||0.4296 mL||2.1480 mL||4.2961 mL|
|10 mM||0.2148 mL||1.0740 mL||2.1480 mL|
. Chresta CM, et al. AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity. Cancer Res, 2010, 70(1), 288-298.
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