For research use only. Not for therapeutic Use.
Cobimetinib hemifumarate (Cat No.:I020490) is a potent and selective inhibitor of MEK1 and MEK2, key enzymes in the MAPK signaling pathway. It is used in the treatment of unresectable or metastatic melanoma with BRAF V600E or V600K mutations. By blocking the activity of MEK1/2, Cobimetinib hemifumarate helps to inhibit tumor cell growth and proliferation. It is often administered in combination with a BRAF inhibitor for enhanced therapeutic efficacy. Cobimetinib hemifumarate has demonstrated promising results in clinical trials and provides a targeted approach for managing advanced melanoma.
| Catalog Number | I020490 |
| CAS Number | 1369665-02-0 |
| Molecular Formula | C₂₁H₂₁F₃IN₃O₂.₁/₂C₄H₄O₄ |
| Purity | ≥95% |
| Storage | Store at -20°C |
| IUPAC Name | (E)-but-2-enedioic acid;[3,4-difluoro-2-(2-fluoro-4-iodoanilino)phenyl]-[3-hydroxy-3-[(2S)-piperidin-2-yl]azetidin-1-yl]methanone |
| InChI | InChI=1S/2C21H21F3IN3O2.C4H4O4/c2*22-14-6-5-13(19(18(14)24)27-16-7-4-12(25)9-15(16)23)20(29)28-10-21(30,11-28)17-3-1-2-8-26-17;5-3(6)1-2-4(7)8/h2*4-7,9,17,26-27,30H,1-3,8,10-11H2;1-2H,(H,5,6)(H,7,8)/b;;2-1+/t2*17-;/m00./s1 |
| InChIKey | RESIMIUSNACMNW-BXRWSSRYSA-N |
| SMILES | C1CCNC(C1)C2(CN(C2)C(=O)C3=C(C(=C(C=C3)F)F)NC4=C(C=C(C=C4)I)F)O.C1CCNC(C1)C2(CN(C2)C(=O)C3=C(C(=C(C=C3)F)F)NC4=C(C=C(C=C4)I)F)O.C(=CC(=O)O)C(=O)O |
| Reference | [1]. Hoeflich KP, et al. Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition. Cancer Res. 2012 Jan 1;72(1):210-9.<br>[2]. Choo EF, et al. PK-PD modeling of combination efficacy effect from administration of the MEK inhibitor GDC-0973 and PI3K inhibitor GDC-0941 in A2058 xenografts. Cancer Chemother Pharmacol. 2013 Jan;71(1):133-43.<br>[3]. Wong H, et al. Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor. Clin Cancer Res. 2012 Jun 1;18(11):3090-9.<br>[4]. Corazao-Rozas P, et al. Mitochondrial oxidative phosphorylation controls cancer cell’s life and death decisions upon exposure to MAPK inhibitors. Oncotarget. 2016 Feb 29. doi: 10.18632/oncotarget.7790. |
