DATASHEET
Formulation
Powder
Storage:
Store in dry, dark place at -20C for 1 year.
Product Information:
Molecular Weight: 462.54
Formula: C25 H30 N6 O3
CAS Number: 1009298-59-2
InChi Key: JUSFANSTBFGBAF-IRXDYDNUSA-N
InChi: InChI=1S/C25H30N6O3/c1-16-14-33-11-9-30(16)23-20-7-8-21(18-5-4-6-19(13-18)24(32)26-3)27-22(20)28-25(29-23)31-10-12-34-15-17(31)2/h4-8,13,16-17H,9-12,14-15H2,1-3H3,(H,26,32)/t16-,17-/m0/s1
Smiles: CNC(=O)C1=CC(=CC=C1)C1C=CC2C(=NC(=NC=2N=1)N1CCOC[C@@H]1C)N1CCOC[C@@H]1C
Purity: 98.0
Solubility: DMSO up to 100 mM
Appearance: Solid Power.
Shelf Life: 1.0 years
Description:
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 α, β, γ, δ = 3.8 µM, >30 µM, >30 µM and >29 µM, respectively) and is inactive against a general panel of over 200 kinases when tested at 10 µM. AZD2014 inhibits both mTORC1 and mTORC2 in vitro (pS6 (S235/236 ) IC50 = 0.2 µM, pAKT (S473) IC50 = 0.08 µM) 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.