Cobimetinib (GDC-0973, RG7420)

Catalog No.S8041 Synonyms: XL518

Cobimetinib (GDC-0973, RG7420) Chemical Structure

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.

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1 Customer Review

  • 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.

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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.
Targets
MEK1 [1]
(Cell-free assay)
4.2 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MDA-MB-231T cells NY\WVmVyTnWwY4Tpc44h[XO|YYm= MWSxJIg> MWHJcohq[mm2aX;uJI9nKE2HSz3t[YRq[XSnZDDFVmshXDJyMj;ZNlA1KHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBOTEFvTVKtNlMyXCClZXzsd{Bi\nSncjCxJIhzKGK7IHntcZVvd2Kub4T0bY5o97zOIFnDOVA:OC5{IH7N NGCw[WczPDlyMES4Oi=>
human COLO205 cells MYDGeY5kfGmxbjDhd5NigQ>? MVjJcohq[mm2aX;uJI9nKEJvcnHmJHY3ODCHIH31eIFvfCCrbjDoeY1idiCFT1zPNlA2KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCxZjDFVmsyN0WUS{KgdIhwe3Cqb4L5cIF1cW:wLDDJR|UxRTFwODDuUS=> MX2yNlMyPTN|Mh?=
human COLO205 cells NGDsXVZRem:uaX\ldoF1cW:wIHHzd4F6 NEPj[nBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPPUG8zODViY3XscJMh\XiycnXzd4lv\yCELYLh[kBXPjByRTDteZRidnRuIFnDOVA:QCCwTR?= MWCyNlMyPTN|Mh?=

... Click to View More Cell Line Experimental Data

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:

[1]

+ Expand
  • Animal Models: Molm-13, Molm-16, MX-1, DLD-1, HCT-116, LoVo, FaDu, 537MEL, A2058, A2058-X1, A375, A375.X1, A427, A549, Calu-6, EBC-1, NCI-H441, NCI-H2122, NCI-H460, NCI-H520.X1, SKOV-3, KP4-X1.1, MiaPaCa-2, 22Rv1, DU-145.X1,S, NCI-H69 xenograft tumors in mice
  • Formulation: --
  • Dosages: 10 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (188.21 mM)
Ethanol 47 mg/mL warmed (88.46 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order:
5% DMSO+30% PEG 300+5% Tween 80+ddH2O
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
Formula

C21H21F3IN3O2

CAS No. 934660-93-2
Storage powder
Synonyms XL518

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02908672 Recruiting Melanoma Hoffmann-La Roche January 2017 Phase 3
NCT03005639 Recruiting Stage IIIB-C Melanoma Inova Health Care Services|Genentech, Inc. December 2016 Phase 2
NCT02968303 Not yet recruiting Melanoma, Malignant, of Soft Parts Radboud University|The Netherlands Cancer Institute|Isala December 2016 Phase 2
NCT02902029 Recruiting Malignant Melanoma University Hospital, Essen November 2016 Phase 2
NCT02876224 Recruiting Colorectal Cancer Hoffmann-La Roche September 2016 Phase 1
NCT02721459 Recruiting Melanoma|Skin Cancer H. Lee Moffitt Cancer Center and Research Institute|Exelixis|Genentech, Inc. August 2016 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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    How to reconstitute the inhibitor for in vivo studies?

  • 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID