Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with an IC50 of 4.2 nM. It is more than 100 times more selective to MEK1 than MEK2, and has no significant inhibitory effect on many other serine-threonine and tyrosine kinases. Cobimetinib can induce apoptosis. Phase 3.

 

Brand: BCM

 

Target: Apoptosis; MEK

 

Signaling Pathways: Apoptosis; MAPK

 

In Vitro: Cobimetinib showed strong inhibitory activity against the growth of a broad group of tumor cell types, particularly against BRAF or KRAS mutant cancer cell lines. The combination administration of GDC-0973 and vemurafenib significantly increased reduced GLUT-1 levels on the cell membrane in all BRAFV600E lines. In combination with GDC-0941, GDC-0973 resulted in reduced viability, pathway inhibition, and increased apoptosis in 888MEL and A2058 cells.

 

Melting Point: 165 - 166°C

 

Boiling Point: 565.9±50.0 °C(Predicted)

 

pKa: 13.13±0.20(Predicted)

 

Solubility: Soluble in DMSO; soluble in Ethanol. Insoluble in Water.

 

GHS: GHS07

 

Isomeric SMILES: C1CCN[C@@H](C1)C2(CN(C2)C(=O)C3=C(C(=C(C=C3)F)F)NC4=C(C=C(C=C4)I)F)O  

 

InChIKey: BSMCAPRUBJMWDF-KRWDZBQOSA-N  

 

InChI: InChI=1S/C21H21F3IN3O2/c22-14-6-5-13(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/h4-7,9,17,26-27,30H,1-3,8,10-11H2/t17-/m0/s1

 

Attribute
[Chem Name]	[3,4-difluoro-2-(2-fluoro-4-iodoanilino)phenyl]-[3-hydroxy-3-[(2S)-piperidin-2-yl]azetidin-1-yl]methanone
[Synonym]	Cobimetinib; GDC-0973; RG7420; XL518
[CAS No.]	934660-93-2
[MDL No.]	MFCD22124461
[Formula]	C21H21F3IN3O2
[Molecular]	531.31
[Form]	Off-white solid powder
[Storage]	Keep in dark place. Inert atmosphere, 2-8°C

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