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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  • 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

GDC-0973 shows strong cellular potency in a broad panel of tumor types, particularly in BRAF (with most of EC50 below 2 μM) or KRAS mutant cancer cell lines. In a panel of cancer cell lines, 80% of BRAF mutant lines (including V600E and non-V600E mutations) are sensitive to GDC-0973, 54% of lines carrying oncogenic mutations in KRAS or NRAS are sensitive, and 35% of the remaining lines are sensitive. GDC-0941 and GDC-0973 act cooperatively to inhibit the viability of all melanoma cell lines tested, 60% of which carry oncogenic mutations in BRAF. Combination of GDC-0941(0.2 μM) and GDC-0973 (10 μM) almost completely suppresses the vitality of 888MEL (BRAFV600E) mutant melanoma cell lines at 4 day. Treatment with GDC-0973 and GDC-0941 results in a combinatorial increase of cellular mediators of apoptosis, such as cleaved PARP and alternatively spliced isoforms of Bim. Transient treatment of 888MEL cells with either single agent GDC-0973 or GDC-0941 results in minimal to no apoptosis induction, whereas GDC-0973 plus GDC-0941 results in a 5-fold increase in apoptosis. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MDA-MB-231T cells NG\xS5BHfW6ldHnvckBie3OjeR?= M2K2dVEhcA>? MULJcohq[mm2aX;uJI9nKE2HSz3t[YRq[XSnZDDFVmshXDJyMj;ZNlA1KHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBOTEFvTVKtNlMyXCClZXzsd{Bi\nSncjCxJIhzKGK7IHntcZVvd2Kub4T0bY5o97zOIFnDOVA:OC5{IH7N MWeyOFkxODR6Nh?=
human COLO205 cells MlrnSpVv[3Srb36gZZN{[Xl? M2rFWGlvcGmkaYTpc44hd2ZiQj3yZYYhXjZyMFWgcZV1[W62IHnuJIh2dWGwIFPPUG8zODViY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJGVTUzFxRWLLNkBxcG:|cHjvdplt[XSrb36sJGlEPTB;MT64JI5O MlXPNlI{OTV|M{K=
human COLO205 cells NH:zUlJRem:uaX\ldoF1cW:wIHHzd4F6 M4[1bGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ1;MU|IxPSClZXzsd{BmgHC{ZYPzbY5oKEJvcnHmJHY3ODCHIH31eIFvfCxiSVO1NF05KG6P MUiyNlMyPTN|Mh?=

... Click to View More Cell Line Experimental Data

In vivo GDC-0973 shows activity in a number of human tumor xenograft models, particularly in models mutant for BRAF. GDC-0973 (5 mg/kg) leads to strong TGI (106%) in the A375.X1 BRAFV600E mutant melanoma xenograft model, accompanied with ~65% p-ERK suppression at 2, 8, and 24 hours. The combination of GDC-0973 (3mg/kg) and GDC-0941 (100mg/kg) leads to a greater tumor response rate for the A375 (BRAFV600E) model, as GDC-0973 results in 70% (7/10) complete responses (CR), GDC-0941 shows lack of TGI, whereas the combination results in 100% (10/10) CRs. [1]

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: Human 888MEL (BRAFV600E) mutant melanoma cell lines
  • Concentrations: ~10 μM
  • Incubation Time: 4 days
  • Method: 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)

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 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
in solvent
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

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID