[CAS NO. 934660-93-2] Cobimetinib (GDC-0973)
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PRODUCTS SPECIFICATIONS [934660-93-2]
Store
Catalog
SLK-S8041
Brand
Selleck
CAS
934660-93-2
DESCRIPTION [934660-93-2]
Overview
| MDL | MFCD22124461 |
|---|---|
| Molecular Weight | 531.31 |
| Molecular Formula | C21H21F3IN3O2 |
| SMILES | C(=O)(C1=C(NC2=C(F)C=C(I)C=C2)C(F)=C(F)C=C1)N3CC(O)(C3)[C@@]4(CCCCN4)[H] |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Description
Cobimetinib (GDC-0973, RG7420) is a potent and highly selective inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Cobimetinib induces . Phase 3.
Targets
| MEK1 [1] (Cell-free assay) |
| 4.2 nM |
In vitro
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.
References
Synonyms
Methanone, [3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl][3-hydroxy-3-(2S)-2-piperidinyl-1-azetidinyl]-
[3,4-Difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl][3-hydroxy-3-(2S)-2-piperidinyl-1-azetidinyl]methanone
XL 518
GDC 0973
Cobimetinib
RG 7421
[3,4-Difluoro-2-(2-fluoro-4-iodoanilino)phenyl]-[3-hydroxy-3-[(2S)-piperidin-2-yl]azetidin-1-yl]methanone
RG7421
RG-7421
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