For research use only. Not for therapeutic Use.
RO4987655（Cat No.:I005266）is an investigational small molecule inhibitor developed by Roche, primarily targeting the protein kinase B (AKT) pathway. AKT is a key regulator of various cellular processes, including cell growth, survival, metabolism, and apoptosis, making it an attractive target for cancer therapy. By inhibiting AKT, RO4987655 aims to block these pro-survival signals, thereby suppressing tumor growth and promoting cancer cell death. Preclinical studies have shown its potential in treating various solid tumors, particularly those with dysregulated AKT signaling. Clinical trials are ongoing to evaluate its safety, efficacy, and potential in cancer treatment.
| Catalog Number | I005266 |
| CAS Number | 874101-00-5 |
| Synonyms | 3,4-difluoro-2-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-5-[(3-oxooxazinan-2-yl)methyl]benzamide |
| Molecular Formula | C20H19F3IN3O5 |
| Purity | ≥95% |
| Target | MEK |
| Solubility | DMSO: ≥ 40 mg/mL |
| Storage | Store at +4C |
| IC50 | 5.2 nM |
| IUPAC Name | 3,4-difluoro-2-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-5-[(3-oxooxazinan-2-yl)methyl]benzamide |
| InChI | InChI=1S/C20H19F3IN3O5/c21-14-9-12(24)3-4-15(14)25-19-13(20(30)26-31-7-5-28)8-11(17(22)18(19)23)10-27-16(29)2-1-6-32-27/h3-4,8-9,25,28H,1-2,5-7,10H2,(H,26,30) |
| InChIKey | FIMYFEGKMOCQKT-UHFFFAOYSA-N |
| SMILES | C1CC(=O)N(OC1)CC2=CC(=C(C(=C2F)F)NC3=C(C=C(C=C3)I)F)C(=O)NOCCO |
| Reference | </br>1:Evaluation of efficacy of a new MEK inhibitor, RO4987655, in human tumor xenografts by [(18)F] FDG-PET imaging combined with proteomic approaches. Tegnebratt T, Ruge E, Bader S, Ishii N, Aida S, Yoshimura Y, Ooi CH, Lu L, Mitsios N, Meresse V, Mulder J, Pawlak M, Venturi M, Tessier J, Stone-Elander S.EJNMMI Res. 2014 Dec;4(1):34. doi: 10.1186/s13550-014-0034-6. Epub 2014 Sep 9. PMID: 26116108 Free PMC Article</br>2:Phase I and pharmacokinetics/pharmacodynamics study of the MEK inhibitor RO4987655 in Japanese patients with advanced solid tumors. Nakamichi S, Nokihara H, Yamamoto N, Yamada Y, Fujiwara Y, Tamura Y, Wakui H, Honda K, Mizugaki H, Kitazono S, Tanabe Y, Asahina H, Yamazaki N, Suzuki S, Matsuoka M, Ogita Y, Tamura T.Invest New Drugs. 2015 Jun;33(3):641-51. doi: 10.1007/s10637-015-0229-3. Epub 2015 Mar 27. PMID: 25809858 </br>3:Phase I expansion and pharmacodynamic study of the oral MEK inhibitor RO4987655 (CH4987655) in selected patients with advanced cancer with RAS-RAF mutations. Zimmer L, Barlesi F, Martinez-Garcia M, Dieras V, Schellens JH, Spano JP, Middleton MR, Calvo E, Paz-Ares L, Larkin J, Pacey S, Venturi M, Kraeber-Bodéré F, Tessier JJ, Eberhardt WE, Paques M, Guarin E, Meresse V, Soria JC.Clin Cancer Res. 2014 Aug 15;20(16):4251-61. doi: 10.1158/1078-0432.CCR-14-0341. Epub 2014 Jun 19. PMID: 24947927 Free Article</br>4:Phase I dose-escalation study of the safety, pharmacokinetics, and pharmacodynamics of the MEK inhibitor RO4987655 (CH4987655) in patients with advanced solid tumors. Leijen S, Middleton MR, Tresca P, Kraeber-Bodéré F, Dieras V, Scheulen ME, Gupta A, Lopez-Valverde V, Xu ZX, Rueger R, Tessier JJ, Shochat E, Blotner S, Naegelen VM, Schellens JH, Eberhardt WE.Clin Cancer Res. 2012 Sep 1;18(17):4794-805. Epub 2012 Jul 5. PMID: 22767668 Free Article |
