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.
CAS Number: 1009298-59-2
Molecular Weight: 462.54
Chemical Name: 3-(2,4-bis((S)-3-methylmorpholino)pyrido[2,3-d]pyrimidin-7-yl)-N-methylbenzamide
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
AZD2014 was used at 2.5-5 µM concentration in vitro and cellular assays.
AZD2014 was orally dosed to mice at 2.5-20 mg/kg once or twice per day to inhibit tumor growth.
- Guichard SM, at al. AZD2014, a dual mTORC1 and mTORC2 inhibitor is differentiated from allosteric inhibitors of mTORC1 in ER+ breast cancer. (2012) AACR Annual Meeting: Chicago, Abstract 917.
- Pike KG, et al. Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: The discovery of AZD8055 and AZD2014. (2013) Bioorg Med Chem Lett. In press.
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