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.
1 Customer Review
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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.
Purity & Quality Control
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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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| 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
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Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
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| NCT01689519 | Active not recruiting | Malignant Melanoma | Hoffmann-La Roche | January 9 2013 | Phase 3 |
| NCT03430947 | Recruiting | Malignant Melanoma Stage IV|BRAF V600 Mutation|Brain Metastases | Technische Universität Dresden | March 7 2018 | Phase 2 |
| NCT03108131 | Recruiting | Malignant Neoplasms of Digestive Organs|Melanoma and Other Malignant Neoplasms of Skin|Appendiceal Adenocarcinoma|Cutaneous Squamous Cell Carcinoma|Small Bowel Adenocarcinoma | M.D. Anderson Cancer Center|Genentech Inc. | April 7 2017 | Phase 2 |
| NCT02788279 | Active not recruiting | Colorectal Cancer | Hoffmann-La Roche | July 5 2016 | Phase 3 |
| NCT03224767 | Recruiting | BRAF V600E Mutation Present|Papillary Craniopharyngioma | Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) | August 4 2017 | Phase 2 |
| NCT03695380 | Not yet recruiting | OVARIAN CANCER | Hoffmann-La Roche | December 31 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.
