Cobimetinib (GDC-0973, RG7420)
Catalog No.S8041 Synonyms: XL518
Molecular Weight(MW): 531.31
Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Phase 3.
3 Customer Reviews
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Three types of selective inhibitors of MAPK signaling produce expected differential kinase inhibition and activation responses in HCT116 colorectal cancer cells. HCT116 cells were treated with 250 nM of GDC-0973, GDC-0623, SCH772984 or DMSO for 1, 4, or 24 h. In the washout samples, cells were drug treated for 24 h, then changed into fresh media and harvested after 0.5 or 2 h. Lysates were used for Western blots of total and phosphorylated MEK, ERK, and RSK; blotting for COX IV was used as the loading control.
Mol Cell Proteomics, 2017, 16(2):265-277. Cobimetinib (GDC-0973, RG7420) purchased from Selleck.
Western blots showing protein changes of p21, p53, cyclin D1, and cyclin E in HCT116 cells after treatment with 1 μM cobimetinib over different timespans.
Cell Physiol Biochem, 2018, 47(2):680-693. Cobimetinib (GDC-0973, RG7420) purchased from Selleck.
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Human-washed platelet aggregation was performed by optical aggregometry following stimulation with U46619 (0.25μM) in the presence or absence of LPS from E. coli O111:B4 (1μg/mL) after 3 min of incubation with Cobimetinib (100μM) before activation with U46619 (0.25μM) (B).
PLoS One, 2017, 12(11):e0186981. Cobimetinib (GDC-0973, RG7420) purchased from Selleck.
Purity & Quality Control
Choose Selective MEK Inhibitors
Biological Activity
| Description | Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Phase 3. | ||||||||||||||||||||||||||||||
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| Targets |
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| In vitro |
Cobimetinib shows strong activity on cell growth inhibtion in a broad panel of tumor types, particularly in BRAF or KRAS mutant cancer cell lines. In combination with GDC-0941, GDC-0973 results in reduced viability, pathway inhibition, and increased apoptosis in 888MEL and A2058 cells. [1] Coadministration of GDC-0973 and vemurafenib significantly increases decreased levels of GLUT-1 on the cellular membrane across all BRAFV600E lines. [2] |
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| Cell Data |
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| In vivo | In mice bearing BRAFV600E and KRAS mutant tumors, Cobimetinib (10 mg/kg, p.o.) produces antitumor efficacy, and the combination of GDC-0973 and GDC-0941 show improved efficacy. [1] In mice bearing drug-resistant A375 xenografts, combination of GDC-0973 and GDC-0941 induces decreased levels of hexokinase II, c-RAF, Ksr and p-MEK protein. [2] |
Protocol
| Animal Research: |
+ Expand
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Solubility (25°C)
| In vitro | DMSO | 100 mg/mL (188.21 mM) |
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| Ethanol | 47 mg/mL warmed (88.46 mM) | |
| Water | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5% DMSO+30% PEG 300+5% Tween 80+ddH2O For best results, use promptly after mixing. |
5mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 531.31 |
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| Formula | C21H21F3IN3O2 |
| CAS No. | 934660-93-2 |
| Storage | powder |
| in solvent | |
| Synonyms | XL518 |
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
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| NCT03732703 | Not yet recruiting | Relapsed Refractory Multiple Myeloma | Multiple Myeloma Research Consortium|AbbVie|Celgene Corporation|Eli Lilly and Company|Genentech Inc.|Janssen LP|Takeda | March 15 2019 | Phase 1|Phase 2 |
| NCT03732703 | Not yet recruiting | Relapsed Refractory Multiple Myeloma | Multiple Myeloma Research Consortium|AbbVie|Celgene Corporation|Eli Lilly and Company|Genentech Inc.|Janssen LP|Takeda | March 15 2019 | Phase 1|Phase 2 |
| NCT03625141 | Recruiting | Metastatic Melanoma | Hoffmann-La Roche | December 13 2018 | Phase 2 |
| NCT03625141 | Recruiting | Metastatic Melanoma | Hoffmann-La Roche | December 13 2018 | Phase 2 |
| NCT03695380 | Recruiting | OVARIAN CANCER | Hoffmann-La Roche | November 2 2018 | Phase 1 |
| NCT03695380 | Recruiting | OVARIAN CANCER | Hoffmann-La Roche | November 2 2018 | Phase 1 |
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
Frequently Asked Questions
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Question 1:
How to reconstitute the inhibitor for in vivo studies?
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Answer:
S8041 can be dissolved in 5% DMSO/30% PEG 300/5% Tween 80/ddH2O at 5 mg/ml clearly and it is ok for both oral gavage and injection.
