Home MAPK MEK inhibitor - Apoptosis related activator Cobimetinib (GDC-0973) For research use only.

Cobimetinib (GDC-0973)

Synonyms: RG7420,XL518

Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, and showing no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Cobimetinib induces apoptosis. Phase 3.

Cobimetinib (GDC-0973) Chemical Structure

Cobimetinib (GDC-0973) Chemical Structure

CAS No. 934660-93-2

Purity & Quality Control

Cobimetinib (GDC-0973) Related Products

Signaling Pathway

MEK Signaling Pathways

MEK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human COLO205 cells Proliferation assay Antiproliferative activity against human COLO205 cells expressing B-raf V600E mutant, IC50=8 nM 22315332
human COLO205 cells Function assay Inhibition of B-raf V600E mutant in human COLO205 cells assessed as reduction of ERK1/ERK2 phosphorylation, IC50=1.8 nM 22315332
human MDA-MB-231T cells Function assay 1 h Inhibition of MEK-mediated ERK T202/Y204 phosphorylation in human MDA-MB-231T cells after 1 hr by immunoblotting， IC50=0.2 nM 24900486
Click to View More Cell Line Experimental Data

Biological Activity

Description Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, and showing no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Cobimetinib induces apoptosis. Phase 3.
Targets
MEK1 [1]
(Cell-free assay)
4.2 nM
In vitro
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]

 
Experimental Result Images Methods Biomarkers Images PMID
Western blot pERK / ERK / MCL-1 / p-MCL1 / BIM / cleaved PARP p-c-RAF / c-RAF / p-MEK / MEK 27765849
Growth inhibition assay Cell viability 28098866
In Vivo
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]
Animal Research 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
Dosages 10 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05756556 Suspended
Melanoma|Malignant Melanoma
ImmVira Pharma Co. Ltd
 June 30 2024 Phase 2
NCT05768178 Recruiting
Solid Tumor|Haematological Malignancy|Melanoma|Thyroid Cancer Papillary|Ovarian Neoplasms|Colorectal Neoplasms|Laryngeal Neoplasms|Carcinoma Non-Small-Cell Lung|Glioma|Multiple Myeloma|Erdheim-Chester Disease|Thyroid Carcinoma Anaplastic
Cancer Research UK|University of Manchester|University of Birmingham|Royal Marsden NHS Foundation Trust|Hoffmann-La Roche
 March 1 2023 Phase 2|Phase 3
NCT04835805 Active not recruiting
Melanoma
Genentech Inc.
 May 13 2021 Phase 1
NCT04109456 Recruiting
Metastatic Melanoma
InxMed (Shanghai) Co. Ltd.
 March 16 2020 Phase 1
NCT04007848 Completed
Disease or R Group Histiocytoses
Assistance Publique - Hôpitaux de Paris
 July 25 2019 Phase 3
NCT03695380 Completed
OVARIAN CANCER
Hoffmann-La Roche
 January 9 2019 Phase 1

Chemical Information & Solubility

Molecular Weight 531.31 Formula

C21H21F3IN3O2
CAS No. 934660-93-2 SDF Download Cobimetinib (GDC-0973) SDF
Smiles C1CCNC(C1)C2(CN(C2)C(=O)C3=C(C(=C(C=C3)F)F)NC4=C(C=C(C=C4)I)F)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (188.21 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 47 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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

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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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