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Cobimetinib

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Purity:100%

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COA HPLC HNMR

Cobimetinib

Catalog No. T3623Cas No. 934660-93-2

Cobimetinib (GDC-0973) is a selective inhibitor of mitogen-activated protein kinase kinase (MEK) (IC50: 0.9 nM). Cobimetinib specifically binds to and inhibits the catalytic activity of MEK1, resulting in inhibition of extracellular signal-related kinase 2 (ERK2) phosphorylation and activation and decreased tumor cell proliferation.

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Pack Size	Price	Availability
1 mg	$34	In Stock
2 mg	$47	In Stock
5 mg	$77	In Stock
10 mg	$97	In Stock
25 mg	$183	In Stock
50 mg	$291	In Stock
100 mg	$477	In Stock
500 mg	Inquiry	In Stock
1 mL x 10 mM (in DMSO)	$90	In Stock

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Product Introduction

Bioactivity

Description	Cobimetinib (GDC-0973) is a selective inhibitor of mitogen-activated protein kinase kinase (MEK) (IC50: 0.9 nM). Cobimetinib specifically binds to and inhibits the catalytic activity of MEK1, resulting in inhibition of extracellular signal-related kinase 2 (ERK2) phosphorylation and activation and decreased tumor cell proliferation.
In vitro	In mice bearing tumors with KRAS and BRAFV600E mutations, Cobimetinib (10 mg/kg, p.o.) has an inhibitory effect on tumor progression. Furthermore, in mice carrying A375 xenografts resistant to treatment, the combined use of Cobimetinib and GDC-0941 further reduces the levels of proteins Hexokinase II, Ksr, c-RAF, and p-MEK.
In vivo	Cobimetinib exhibits potent inhibitory effects on the growth of various tumor cells, particularly those with KRAS or BRAF mutations. When used in conjunction with GDC-0941, cobimetinib significantly reduces the viability of 888MEL and A2058 cells, inhibits pathways, and increases apoptosis. Additionally, the combination of cobimetinib and vemurafenib markedly intensifies the reduction of GLUT-1 on the cell membranes across all BRAFV600E cell lines. [1]
Cell Research	Cells are plated in quadruplicate at a density of 3,000 per well in 384-well plates in normal growth medium and allowed to adhere overnight. Compounds are added in 10 concentrations based on a 3-fold dilution series. Cell viability is measured 72 h later using the CellTiter-Glo Luminescent Cell Viability Assay.(Only for Reference)
Alias	RG7420, XL518, GDC-0973

Chemical Properties

Molecular Weight	531.31
Formula	C21H21F3IN3O2
Cas No.	934660-93-2

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 44 mg/mL (82.8 mM)

DMSO: 16.67 mg/mL (31.37 mM)

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.8821 mL	9.4107 mL	18.8214 mL	94.1070 mL
5 mM	0.3764 mL	1.8821 mL	3.7643 mL	18.8214 mL
10 mM	0.1882 mL	0.9411 mL	1.8821 mL	9.4107 mL
20 mM	0.0941 mL	0.4705 mL	0.9411 mL	4.7054 mL

Ethanol

	1mg	5mg	10mg	50mg
50 mM	0.0376 mL	0.1882 mL	0.3764 mL	1.8821 mL
100 mM	0.0188 mL	0.0941 mL	0.1882 mL	0.9411 mL

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In Vivo Formulation Calculator (Clear solution)

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

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Tech Support

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