Cellagentech/AZD8055 | mTOR inhibitor/C2955-5/5 mg (powder)
Product Description
AZD8055 is a potent and orally bioavailable ATP-competitive inhibitor of mTOR kinase with an IC50 of 0.8 nM. It inhibits both mTORC1 and mTORC2. AZD8055 shows excellent selectivity (1,000-fold) against all class I PI3K isoforms and other members of the PI3K-like kinase family. Furthermore, AZD8055 showed no significant activity against a panel of 260 kinases at concentrations up to 10 µM [1]. The serine/threonine kinase mTOR is crucial for cell growth and proliferation. It regulates cap-dependent translation through the mTORC1 complex and Akt activation through the mTORC2 complex. AZD8055 inhibits the phosphorylation of mTORC1 substrates p70S6K and 4E-BP1 as well as the phosphorylation of the mTORC2 substrate AKT. AZD8055 potently inhibits proliferation, induces autophagy and apoptosis in different cells. In vivo, AZD8055 induces a dose-dependent pharmacodynamic effect on phosphorylated S6 and phosphorylated AKT and results in significant tumor growth inhibition and/or regression in xenografts representing a broad range of tumor types [1-4].
Technical information:
| Chemical Formula: | C25H31N5O4 | |
| CAS #: | 1009298-09-2 | |
| Molecular Weight: | 465.54 | |
| Purity: | > 98% | |
| Appearance: | White | |
| Chemical Name: | (5-(2,4-bis((S)-3-methylmorpholino)pyrido[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol | |
| Solubility: | Up to 22 mM in DMSO | |
| Synonyms: | AZD8055, AZD-8055 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature. Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | 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):288-98. Pubmed ID: 20028854 |
| 2. | Sini P, et al. Simultaneous inhibition of mTORC1 and mTORC2 by mTOR kinase inhibitor AZD8055 induces autophagy and cell death in cancer cells. Autophagy. 2010. 6(4). Pubmed ID: 20364113 |
| 3. | Willems L, et al. The dual mTORC1 and mTORC2 inhibitor AZD8055 has anti-tumor activity in acute myeloid leukemia. . Leukemia. 2012. 26(6):1195-202. Pubmed ID: 22143671 |
| 4. | Naing A,et al. Safety, tolerability, pharmacokinetics and pharmacodynamics of AZD8055 in advanced solid tumours and lymphoma. Br J Cancer. 2012. 107(7):1093-9. Pubmed ID: 22935583 |
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