Cobimetinib

  • Chemical Properties
CAS No. 934660-93-2 Cat. No. BCP05208
Name Cobimetinib
Synonyms GDC-0973;XL-518;GDC 0973;XL 518;GDC0973;XL518;
Formula C21H21F3IN3O2 M. Wt 531.31
  • Biological Activity
Description in vitro: The combination of GDC-0973 with the PI3K inhibitor GDC-0941 resulted in combination efficacy in vitro and in vivo via induction of biomarkers associated with apoptosis, including Bcl-2 family proapoptotic regulators . in vivo: The population rate constants associated with tumor growth inhibition for GDC-0973 and GDC-0941 were 0.00102 and 0000651 μM(-1) h(-1), respectively. Using the model based on single-agent and QD combination efficacy data, simulations adequately described the tumor growth from the Q3D combination regimen . Following single doses of GDC-0973, estimated in vivo IC(50) values of %pERK decrease based on tumor concentrations in xenograft mice were 0.78 (WM-266-4) and 0.52 μmol/L (A375).
Related Products 1369665-02-0(Cobimetinib hemifumarate)
Pathways MAPK Pathway 
Targets MEK/ERK 

Structure

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