AZD2014 --- mTOR Inhibitor [1009298-59-2] [1009298-59-2]

Bioss

AZD2014 --- mTOR Inhibitor [1009298-59-2] [1009298-59-2]

16

1009298-59-2

Research Use Only

Unconjugated

98 - 98.0

C25 H30 N6 O3

462.54

AZD2014 is a highly potent, selective and ATP-competitive mTOR inhibitor (IC50 = 2.8 nM). It displays a high level of selectivity against other members of the PIKK family (IC50 against PI3K isoforms alpha, beta, gamma, delta = 3.8 microM, >30 microM, >30 microM and >29 microM, respectively) and is inactive against a general panel of over 200 kinases when tested at 10 microM. AZD2014 inhibits both mTORC1 and mTORC2 in vitro (pS6 (S235/236 ) IC50 = 0.2 microM, pAKT (S473) IC50 = 0.08 microM) and has shown dose-dependent tumor growth inhibition in a mouse MCF7 xenograft model alongside modulation of mTORC1 and mTORC2 biomarkers. Different from AZD8055, AZD2014 shows consistent exposure in rodents and a low turnover in human hepatocyte incubations. It is in phase I clinical development for advanced solid malignancies.

CNC(=O)C1=CC(=CC=C1)C1C=CC2C(=NC(=NC=2N=1)N1CCOC[C@@H]1C)N1CCOC[C@@H]1C

-20°C

12161509