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Chemdea |
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AZD8055 – mTOR Inhibitor |
Catalog # CD0348 |
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Price: 1 mg - $65;
5 mg - $95; 10 mg - $145; 25 mg - $295; 50 mg - $395; 100 mg - $650, 200 mg -
$1095 |
Availability: In stock |
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5-[2,4-Bis[(3S)-3-methyl-4-morpholinyl]pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol
Yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. Purity > 99% by HPLC. Optically pure. CAS# 1009298-09-2. Solubility: DMSO (100 mg/mL). Molecular Formula: C25H31N5O4. Molecular Weight: 465.56.
AZD8055 is a novel ATP-competitive inhibitor of mTOR kinase (both complexes mTORC1 and mTORC2) with an IC50 of 0.8 nM. It shows 1000 fold selectivity against all PI3K isoforms and other members of the PI3K-like family. Furthermore AZD8055 does not show significant activity against a 260-membered kinase panel (IC50 > 10 mM). AZD8055 inhibits the phosphorylation of mTORC1 substrates p70S6K and 4E-BP1 as well as phosphorylation of the mTORC2 substrate AKT and downstream proteins. The rapamycin-resistant T37/46 phosphorylation sites on 4E-BP1 were fully inhibited by AZD8055, resulting in significant inhibition of cap-dependent translation. In vitro, AZD8055 potently inhibits proliferation and induces autophagy in H838 and A549 cells. In vivo, AZD8055 induces a dose-dependent pharmacodynamic effect on phosphorylated S6 and phosphorylated AKT at plasma concentrations leading to tumor growth inhibition. Notably, AZD8055 results in significant growth inhibition and/or regression in xenografts, representing a broad range of human tumor types.
References: 1. Chresta, C. M., et al. Cancer Res. 2010, 70, 288; 2. Sini, P. et al. Autophagy. 2010, 6, 553. |
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CHEMDEA; |