product name Cobimetinib (GDC-0973)
Description: Cobimetinib, also known as GDC-0973, RG7420 or XL-518, is a highly potent and selective MEK1 inhibitor with IC50 of 4.2 nM. It is an orally bioavailable small-molecule inhibitor of MEK1 with potential antineoplastic activity. GDC-0973 specifically binds to and inhibits the catalytic activity of MEK1, resulting in inhibition of extracellular signal-related kinase 2 (ERK2) phosphorylation and activation and decreased tumor cell proliferation.
References: Cancer Res. 2012 Jan 1;72(1):210-9; JEJNMMI Res. 2012 May 31;2(1):22.
531.31
Formula
C21H21F3IN3O2
CAS No.
934660-93-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (188.2 mM)
Water: <1 mg/mL
Ethanol: 47 mg/mL (88.46 mM)
Solubility (In vivo)
5% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5 mg/mL
Synonyms
XL518, GDC-0973, RG7420
other peoduct :
| In Vitro |
In vitro activity: Cobimetinib shows strong activity on cell growth inhibtion in a broad panel of tumor types, particularly in BRAF or KRAS mutant cancer cell lines. In combination with GDC-0941, GDC-0973 results in reduced viability, pathway inhibition, and increased apoptosis in 888MEL and A2058 cells. Coadministration of GDC-0973 and vemurafenib significantly increases decreased levels of GLUT-1 on the cellular membrane across all BRAFV600E lines. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In mice bearing BRAFV600E and KRAS mutant tumors, Cobimetinib (10 mg/kg, p.o.) produces antitumor efficacy, and the combination of GDC-0973 and GDC-0941 show improved efficacy. In mice bearing drug-resistant A375 xenografts, combination of GDC-0973 and GDC-0941 induces decreased levels of hexokinase II, c-RAF, Ksr and p-MEK protein |
| Animal model | |
| Formulation & Dosage | |
| References | Cancer Res. 2012 Jan 1;72(1):210-9; JEJNMMI Res. 2012 May 31;2(1):22. |
