Cobimetinib(GDC-0973; XL518)
Cat. No.: DC4177
Featured
Chemical Structure
934660-93-2
We are official vendor of:
More than 5000 active chemicals with high quality for research!
Field of application
GDC-0973 is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase, also known as MEK, a serine/threonine kinase that is a component of the RAS/RAF/MEK/ERK pathway.
| Cas No.: |
934660-93-2 |
| Chemical Name: |
Cobimetinib |
| Synonyms: |
XL518;Cobimetinib;[3,4-difluoro-2-(2-fluoro-4-iodoanilino)phenyl]-[3-hydroxy-3-[(2S)-piperidin-2-yl]azetidin-1-yl]methanone;GDC-0973;GDC-0973 (XL-518);GDC-0973(XL518,RG7420);[3,4-Bis(Fluoranyl)-2-[(2-Fluoranyl-4-Iodanyl-Phenyl)amino]phenyl]-[3-Oxidanyl-3-[(2s)-Piperidin-2-Yl]azetidin-1-Yl]methanone;EUI;GDC 0973;XL-518;[3,4-Difluoro-2-(2-fluoro-4-methylanilino)phenyl]-[3-hydroxy-3-[(2S)-piperidin-2-yl]azetidin-1-yl]me |
| SMILES: |
FC1=C(C([H])=C([H])C(=C1N([H])C1C([H])=C([H])C(C([H])([H])[H])=C([H])C=1F)C(N1C([H])([H])C(C1([H])[H])([C@]1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])N1[H])O[H])=O)F |
| Formula: |
C22H24F3N3O2 |
| M.Wt: |
419.4401 |
| Sotrage: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: |
Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK inhibitor with an IC50 of 4.2 nM for MEK1. |
| In Vivo: |
In the NCI-H2122 KRASG12C mutant non-small cell lung carcinoma (NSCLC) xenograft model, treatment with up to 5 mg/kg Cobimetinib (GDC-0973) lead to moderate TGI and at 10 mg/kg approaches tumor stasis[1]. GDC-0973 and GDC-0941 are administered to A2058 tumor-bearing mice daily (QD) or every third day (Q3D) either as single agents or in combination. The population rate constants associated with tumor growth inhibition for GDC-0973 and GDC-0941 are 0.00102 and 0000651 μM-1 h-1, respectively[2]. Following single doses of GDC-0973 (1, 3, or 10 mg/kg, p.o.) estimated in vivo IC50 values of %pERK decrease based on tumor concentrations in xenograft mice are 0.78 (WM-266-4) and 0.52 μM (A375)[3]. |
| In Vitro: |
The EC50 values of Cobimetinib (GDC-0973) for 888MEL and A2058 cells are 0.2 μM, 10 μM, respectivelly. Melanoma cells are treated with EC50 concentration of MEK and PI3K inhibitors for 24 hours (888MEL: 0.05 μM GDC-0973, 2.5 μM GDC-0941; A2058: 2.5 μM GDC-0973, 2.5 μM GDC-0941)[1]. Mitochondrial OXPHOS limits cell death induced by cobimetinib (100 nM) in melanoma with constitutive MAPK activation in A375 cells[4]. |
MSDS
COA
| LOT NO. |
DOWNLOAD |
|
|
| 2018-0101 |
|
| 2018-0101 |
|
Get Quote
