azd8055

Description: AZD8055 is a novel, potent selective, and orally bioavailable ATP-competitive mTOR (mammalian target of rapamycin) inhibitor with potential anticancer activity. It inhibits mTOR with an IC50 of 0.8 nM in MDA-MB-468 cells and has excellent selectivity (?1, 000-fold) against PI3K isoforms and ATM/DNA-PK. As an mTOR inhibitor, AZD-8055 showed potent antineoplastic activity by inhibiting the serine/threonine kinase activity of mTOR, resulting in decreased expression of mRNAs necessary for cell cycle progression, which may induce cell cycle arrest and tumor cell apoptosis. mTOR phosphorylates transcription factors, such as S6K1 and 4E-BP1, which stimulate protein synthesis and regulate cell growth, proliferation, motility, and survival.

References: Cancer Res. 2010 Jan 1; 70(1):288-98; Br J Cancer. 2011 Mar 29; 104(7):1116-25.