AZD-2014

• CAT Number: I000107
• CAS Number: 1009298-59-2
• Molecular Formula: C₂₅H₃₀N₆O₃
• Molecular Weight: 462.54
• Purity: ≥95%
• Target: mTOR
• Solubility: in DMSO > 10 mM
• Storage: 3 years -20℃ powder
• IC50: 2.8 nM
• IUPAC Name: 3-[2,4-bis[(3S)-3-methylmorpholin-4-yl]pyrido[2,3-d]pyrimidin-7-yl]-N-methylbenzamide
• 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
• InChIKey: JUSFANSTBFGBAF-IRXDYDNUSA-N
• SMILES: CC1COCCN1C2=NC(=NC3=C2C=CC(=N3)C4=CC(=CC=C4)C(=O)NC)N5CCOCC5C

AZD-2014 (Cat.No:I000107) is a selective inhibitor of mTOR kinase, which is a key regulator of cell growth, proliferation, and survival. It has shown promise in preclinical and clinical studies for the treatment of various cancers. AZD-2014 has also demonstrated potential for the treatment of tuberous sclerosis complex and other disorders related to abnormal mTOR activation.

Reference

1:Rapamycin-insensitive companion of mTOR (RICTOR) amplification defines a subset of advanced gastric cancer and is sensitive to AZD2014-mediated mTORC1/2 inhibition. Kim ST, Kim SY, Klempner SJ, Yoon J, Kim N, Ahn S, Bang H, Kim KM, Park W, Park SH, Park JO, Park YS, Lim HY, Lee SH, Park K, Kang WK, Lee J.Ann Oncol. 2017 Mar 1;28(3):547-554. doi: 10.1093/annonc/mdw669. PMID: 28028034 2:AZD2014 Radiosensitizes Oral Squamous Cell Carcinoma by Inhibiting AKT/mTOR Axis and Inducing G1/G2/M Cell Cycle Arrest. Yu CC, Huang HB, Hung SK, Liao HF, Lee CC, Lin HY, Li SC, Ho HC, Hung CL, Su YC.PLoS One. 2016 Mar 31;11(3):e0151942. doi: 10.1371/journal.pone.0151942. eCollection 2016. PMID: 27031247 Free PMC Article3:The novel combination of dual mTOR inhibitor AZD2014 and pan-PIM inhibitor AZD1208 inhibits growth in acute myeloid leukemia via HSF pathway suppression. Harada M, Benito J, Yamamoto S, Kaur S, Arslan D, Ramirez S, Jacamo R, Platanias L, Matsushita H, Fujimura T, Kazuno S, Kojima K, Tabe Y, Konopleva M.Oncotarget. 2015 Nov 10;6(35):37930-47. doi: 10.18632/oncotarget.6122. PMID: 26473447 Free PMC Article4:A Randomised Phase 2 Study of AZD2014 Versus Everolimus in Patients with VEGF-Refractory Metastatic Clear Cell Renal Cancer. Powles T, Wheater M, Din O, Geldart T, Boleti E, Stockdale A, Sundar S, Robinson A, Ahmed I, Wimalasingham A, Burke W, Sarker SJ, Hussain S, Ralph C.Eur Urol. 2016 Mar;69(3):450-6. doi: 10.1016/j.eururo.2015.08.035. Epub 2015 Sep 11. PMID: 26364551 5:AZD2014, an Inhibitor of mTORC1 and mTORC2, Is Highly Effective in ER+ Breast Cancer When Administered Using Intermittent or Continuous Schedules. Guichard SM, Curwen J, Bihani T, D/’Cruz CM, Yates JW, Grondine M, Howard Z, Davies BR, Bigley G, Klinowska T, Pike KG, Pass M, Chresta CM, Polanska UM, McEwen R, Delpuech O, Green S, Cosulich SC.Mol Cancer Ther. 2015 Nov;14(11):2508-18. doi: 10.1158/1535-7163.MCT-15-0365. Epub 2015 Sep 10. PMID: 26358751 Free Article6:First-in-Human Pharmacokinetic and Pharmacodynamic Study of the Dual m-TORC 1/2 Inhibitor AZD2014. Basu B, Dean E, Puglisi M, Greystoke A, Ong M, Burke W, Cavallin M, Bigley G, Womack C, Harrington EA, Green S, Oelmann E, de Bono JS, Ranson M, Banerji U.Clin Cancer Res. 2015 Aug 1;21(15):3412-9. doi: 10.1158/1078-0432.CCR-14-2422. Epub 2015 Mar 24. PMID: 25805799 Free PMC Article7:Dramatic antitumor effects of the dual mTORC1 and mTORC2 inhibitor AZD2014 in hepatocellular carcinoma. Liao H, Huang Y, Guo B, Liang B, Liu X, Ou H, Jiang C, Li X, Yang D.Am J Cancer Res. 2014 Dec 15;5(1):125-39. eCollection 2015. PMID: 25628925 Free PMC Article8:The mTORC1/mTORC2 inhibitor AZD2014 enhances the radiosensitivity of glioblastoma stem-like cells. Kahn J, Hayman TJ, Jamal M, Rath BH, Kramp T, Camphausen K, Tofilon PJ.Neuro Oncol. 2014 Jan;16(1):29-37. doi: 10.1093/neuonc/not139. Epub 2013 Dec 4. PMID: 24311635 Free PMC Article9:Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014. Pike KG, Malagu K, Hummersone MG, Menear KA, Duggan HM, Gomez S, Martin NM, Ruston L, Pass SL, Pass M.Bioorg Med Chem Lett. 2013 Mar 1;23(5):1212-6. doi: 10.1016/j.bmcl.2013.01.019. Epub 2013 Jan 18. PMID: 23375793