Name: Cobimetinib (GDC-0973)
Brand: Selleck Chemicals
SKU: S8041
Availability: InStock
Rating: 5 (117 reviews)

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Quality Control

Batch: Purity: 99.86%

99.86

Related Targets	ERK p38 MAPK Raf JNK Ras KRas S6 Kinase MAP4K TAK1 Mixed Lineage Kinase
Other MEK Inhibitors	PD0325901 (Mirdametinib) U0126-EtOH PD 98059 CI-1040 (PD184352) (E/Z)-BIX02189 Pimasertib (AS-703026) Refametinib (RDEA119) TAK-733 AZD8330 GDC-0623

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (188.21 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 47 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 30%PEG300 2 5%Tween80 3 60%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.41mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 300 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 600 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.41mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	531.31	Formula	C₂₁H₂₁F₃IN₃O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	934660-93-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	RG7420,XL518			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

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	MEK1 (Cell-free assay) 4.2 nM
In vitro	Cobimetinib (GDC-0973) 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, it results in reduced viability, pathway inhibition, and increased apoptosis in 888MEL and A2058 cells.
In vivo	In mice bearing BRAFV600E and KRAS mutant tumors, Cobimetinib (GDC-0973) (10 mg/kg, p.o.) produces antitumor efficacy, and the combination of this compound and GDC-0941 show improved efficacy. In mice bearing drug-resistant A375 xenografts, the combination of it and GDC-0941 induces decreased levels of hexokinase II, c-RAF, Ksr and p-MEK protein.
References	[1] https://pubmed.ncbi.nlm.nih.gov/22084396/ [2] https://pubmed.ncbi.nlm.nih.gov/22651703/

Applications

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

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-11-24)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05768178	RECRUITING	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; Solid Tumour	Cancer Research UK	2023-03-01	PHASE2; PHASE3
NCT05722886	RECRUITING	Haematological Malignancy; Solid Tumour	Cancer Research UK	2023-03-01	PHASE2; PHASE3
NCT07449754	RECRUITING	Advanced or Metastatic Melanoma	Hanmi Pharmaceutical Company Limited	2026-02-12	PHASE2
NCT04341181	RECRUITING	Cancer; Tumors; Neoplasms; Neoplasia	Ulrik Lassen	2020-08-24	PHASE2
NCT03202940	ACTIVE_NOT_RECRUITING	Non-small Cell Lung Cancer	Massachusetts General Hospital	2017-09-14	PHASE1; PHASE2
NCT03768063	ACTIVE_NOT_RECRUITING	Cancer	Hoffmann-La Roche	2019-02-28	PHASE3

Tech Support

Handling Instructions

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

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
How to reconstitute it for in vivo studies?

Answer:
It can be dissolved in 5% DMSO/30% PEG 300/5% Tween 80/ddH2O at 5 mg/ml clearly and is suitable for both oral gavage and injection.

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Cobimetinib (GDC-0973) MEK1 inhibitor

Chemical Structure

Molecular Weight: 531.31