AZD8055 --- mTOR Inhibitor

Bioss Antibodies

AZD8055 --- mTOR Inhibitor [1009298-09-2]

16

Research Use Only

98.0

AZD8055 is a highly potent, selective and ATP-competitive mTOR inhibitor (IC50 = 0.8 nM). It has >1, 000-fold selectivity against all PI3K isoforms (alpha, beta, gamma, delta) and other members of the PI3K-like kinase family (ATM and DNA-PK). It has no significant activity against a panel of 260 kinases at concentrations up to 10 microM. AZD8055 inhibits the phosphorylation of mTORC1 downstream targets (p70S6K and 4E-BP1) as well as phosphorylation of the mTORC2 downstream proteins (e.g., Akt). 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 of U87MG, A549 and H838 cells with IC50 of 53, 50, and 20 nM, respectively. It also induces autophagy and increases 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. It also 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 was previously evaluated in a phase I clinical study in patients with advanced tumors.

-20°C

51202000