For research use only. Not for therapeutic Use.
BEZ235 (NVP-BEZ235)（Cat No.:I005455）is a dual inhibitor of phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR), two key components of the PI3K/Akt/mTOR signaling pathway that regulates cell growth, survival, and metabolism. By targeting both PI3K and mTOR, BEZ235 disrupts cancer cell proliferation and induces apoptosis, making it a promising therapeutic candidate in oncology. It has shown efficacy in preclinical studies for a range of cancers, including breast and prostate cancers. BEZ235 is being investigated in clinical trials for its potential in treating tumors with hyperactivated PI3K/mTOR signaling.
| Catalog Number | I005455 |
| CAS Number | 915019-65-7 |
| Synonyms | 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-ylimidazo[4,5-c]quinolin-1-yl)phenyl]propanenitrile |
| Molecular Formula | C₃₀H₂₃N₅O |
| Purity | ≥95% |
| Target | Autophagy |
| Solubility | DMSO: ≤ 8.75 mg/mL |
| Storage | 3 years -20C powder |
| IC50 | 4 nM/5 nM/7 nM/75 nM/6 nM(p110α/γ/δ/β/mTOR) |
| IUPAC Name | 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-ylimidazo[4,5-c]quinolin-1-yl)phenyl]propanenitrile |
| InChI | InChI=1S/C30H23N5O/c1-30(2,18-31)22-9-11-23(12-10-22)35-28-24-15-19(21-14-20-6-4-5-7-25(20)32-16-21)8-13-26(24)33-17-27(28)34(3)29(35)36/h4-17H,1-3H3 |
| InChIKey | JOGKUKXHTYWRGZ-UHFFFAOYSA-N |
| SMILES | CC(C)(C#N)C1=CC=C(C=C1)N2C3=C4C=C(C=CC4=NC=C3N(C2=O)C)C5=CC6=CC=CC=C6N=C5 |
| Reference | </br>1:The effect of rapamycin, NVP-BEZ235, aspirin, and metformin on PI3K/AKT/mTOR signaling pathway of PIK3CA-related overgrowth spectrum (PROS). Suzuki Y, Enokido Y, Yamada K, Inaba M, Kuwata K, Hanada N, Morishita T, Mizuno S, Wakamatsu N.Oncotarget. 2017 May 2. doi: 10.18632/oncotarget.17566. [Epub ahead of print] PMID: 28525374 </br>2:Retinoblastoma cells activate the AKT pathway and are vulnerable to the PI3K/mTOR inhibitor NVP-BEZ235. Xie C, Freeman MJ, Lu H, Wang X, Forster CL, Sarver AL, Hallstrom TC.Oncotarget. 2017 Apr 8. doi: 10.18632/oncotarget.16970. [Epub ahead of print] PMID: 28445155 Free Article</br>3:Efficacy of the dual PI3K and mTOR inhibitor NVP-BEZ235 in combination with imatinib mesylate against chronic myelogenous leukemia cell lines. Xin P, Li C, Zheng Y, Peng Q, Xiao H, Huang Y, Zhu X.Drug Des Devel Ther. 2017 Apr 3;11:1115-1126. doi: 10.2147/DDDT.S132092. eCollection 2017. PMID: 28435223 Free PMC Article</br>4:A Phase Ib Study of the Dual PI3K/mTOR Inhibitor Dactolisib (BEZ235) Combined with Everolimus in Patients with Advanced Solid Malignancies. Wise-Draper TM, Moorthy G, Salkeni MA, Karim NA, Thomas HE, Mercer CA, Beg MS, O/’Gara S, Olowokure O, Fathallah H, Kozma SC, Thomas G, Rixe O, Desai P, Morris JC.Target Oncol. 2017 Mar 29. doi: 10.1007/s11523-017-0482-9. [Epub ahead of print] PMID: 28357727 </br>5:A Phase I Study of Abiraterone Acetate Combined with BEZ235, a Dual PI3K/mTOR Inhibitor, in Metastatic Castration Resistant Prostate Cancer. Wei XX, Hsieh AC, Kim W, Friedlander T, Lin AM, Louttit M, Ryan CJ.Oncologist. 2017 May;22(5):503-e43. doi: 10.1634/theoncologist.2016-0432. Epub 2017 Mar 17. PMID: 28314838 Free PMC Article</br>6:Phase Ib dose-finding study of abiraterone acetate plus buparlisib (BKM120) or dactolisib (BEZ235) in patients with castration-resistant prostate cancer. Massard C, Chi KN, Castellano D, de Bono J, Gravis G, Dirix L, Machiels JP, Mita A, Gonzalez BM, Turri S, Maier J, Csonka D, Chakravartty A, Fizazi K.Eur J Cancer. 2017 May;76:36-44. doi: 10.1016/j.ejca.2017.01.024. Epub 2017 Mar 20. PMID: 28282611 </br>7:PI3K/mTOR dual inhibitor BEZ235 and histone deacetylase inhibitor Trichostatin A synergistically exert anti-tumor activity in breast cancer. Chen L, Jin T, Zhu K, Piao Y, Quan T, Quan C, Lin Z.Oncotarget. 2017 Feb 14;8(7):11937-11949. doi: 10.18632/oncotarget.14442. PMID: 28060760 Free PMC Article</br>8:The PI3K/mTOR dual inhibitor BEZ235 suppresses proliferation and migration and reverses multidrug resistance in acute myeloid leukemia. Deng L, Jiang L, Lin XH, Tseng KF, Liu Y, Zhang X, Dong RH, Lu ZG, Wang XJ.Acta Pharmacol Sin. 2017 Mar;38(3):382-391. doi: 10.1038/aps.2016.121. Epub 2017 Jan 2. PMID: 28042875 Free PMC Article</br>9:Dual blocking of PI3K and mTOR signaling by NVP-BEZ235 inhibits proliferation in cervical carcinoma cells and enhances therapeutic response. Xie G, Wang Z, Chen Y, Zhang S, Feng L, Meng F, Yu Z.Cancer Lett. 2017 Mar 1;388:12-20. doi: 10.1016/j.canlet.2016.11.024. Epub 2016 Nov 25. PMID: 27894954 </br>10:Kinetic modelling of in vitro data of PI3K, mTOR1, PTEN enzymes and on-target inhibitors Rapamycin, BEZ235, and LY294002. Goltsov A, Tashkandi G, Langdon SP, Harrison DJ, Bown JL.Eur J Pharm Sci. 2017 Jan 15;97:170-181. doi: 10.1016/j.ejps.2016.11.008. Epub 2016 Nov 8. PMID: 27832967 |
