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Cobimetinib

Catalog No. T3623 CAS 934660-93-2

Synonyms: RG7420, XL518, GDC-0973

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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Cobimetinib, CAS 934660-93-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
2 mg	In stock	$ 47.00
5 mg	In stock	$ 77.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 183.00
50 mg	In stock	$ 291.00
100 mg	In stock	$ 477.00
500 mg	In stock	Inquiry
1 mL * 10 mM (in DMSO)	In stock	$ 90.00

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Purity: 100%

Purity: 99.98%

Purity: 98.93%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

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.
Targets&IC50	MEK:0.9 nM
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)

Synonyms	RG7420, XL518, GDC-0973
Molecular Weight	531.31
Formula	C21H21F3IN3O2
CAS No.	934660-93-2

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: 93 mg/mL (175 mM)

References and Literature

1. Hoeflich KP, et al. Cancer Res. 2012, 72(1), 210-219. 2. Baudy AR, et al. EJNMMI Res. 2012, 2(1), 22.

Citations

1. Meng Y, Lv T, Zhang J, et al.Temporospatial inhibition of Erk signaling is required for lymphatic valve formation.Signal Transduction and Targeted Therapy.2023, 8(1): 342.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Inhibitor Library Kinase Inhibitor Library Highly Selective Inhibitor Library EMA Approved Drug Library Anti-Cancer Clinical Compound Library FDA-Approved Kinase Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library Drug Repurposing Compound Library

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Keywords

Cobimetinib 934660-93-2 Apoptosis MAPK MEK XL 518 RG-7420 GDC0973 Inhibitor inhibit MAP2K MAPKK Mitogen-activated protein kinase kinase XL-518 GDC 0973 RG7420 RG 7420 XL518 GDC-0973 inhibitor

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