Product Name :
AZD2014 — mTOR Inhibitor
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.
CAS:
1009298-59-2
Molecular Weight:
462.54
Formula:
C25H30N6O3
Chemical Name:
3-(2,4-bis((S)-3-methylmorpholino)pyrido[2,3-d]pyrimidin-7-yl)-N-methylbenzamide
Smiles :
CNC(=O)C1=CC(=CC=C1)C1=CC=C2C(=N1)N=C(N=C2N1CCOC[C@@H]1C)N1CCOC[C@@H]1C
InChiKey:
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
Purity:
≥98% (or refer to the Certificate of Analysis)
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.{{Tacrine} medchemexpress|{Tacrine} Neuronal Signaling|{Tacrine} Protocol|{Tacrine} References|{Tacrine} supplier|{Tacrine} Cancer}
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
AZD2014 is a highly potent, selective and ATP-competitive mTOR inhibitor (IC50 = 2.{{Dehydroabietic acid} MedChemExpress|{Dehydroabietic acid} Bacterial|{Dehydroabietic acid} Purity & Documentation|{Dehydroabietic acid} Description|{Dehydroabietic acid} custom synthesis|{Dehydroabietic acid} Epigenetics} 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.|Product information|CAS Number: 1009298-59-2|Molecular Weight: 462.54|Formula: C25H30N6O3|Chemical Name: 3-(2,4-bis((S)-3-methylmorpholino)pyrido[2,3-d]pyrimidin-7-yl)-N-methylbenzamide|Smiles: CNC(=O)C1=CC(=CC=C1)C1=CC=C2C(=N1)N=C(N=C2N1CCOC[C@@H]1C)N1CCOC[C@@H]1C|InChiKey: 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|Technical Data|Appearance: Solid Power.PMID:24633055 |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|In Vitro:|AZD2014 was used at 2.5-5 µM concentration in vitro and cellular assays.|In Vivo:|AZD2014 was orally dosed to mice at 2.5-20 mg/kg once or twice per day to inhibit tumor growth.|References:|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.Products are for research use only. Not for human use.|Documents||