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Cobimetinib (GDC-0973, RG7420)

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Synonyms ：
GDC0973;XL
Appearance ：
Chemical Formula ：
C21H21F3IN3O2
Solubility ：
DMSO 100 mg/mL (188.21 mM)
Molecular Weight ：
531.31
Storage and Stability ：
in stock
CAS No. ：
934660-93-2
Purity ：
98%
Introduction
Cobimetinib(GDC-0973; XL518) is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase.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).

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