Cat. No.: HY-13064A

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Cobimetinib hemifumarate

(Synonyms: GDC-0973 hemifumarate; XL-518 hemifumarate)

63 Cited Publications

Customer Review

Based on 63 publication(s) in Google Scholar

Cobimetinib hemifumarate is a novel selective MEK1 inhibitor, and the IC₅₀ value against MEK1 is 4.2 nM.

For research use only. We do not sell to patients.

Purity: 99.68%
CAS No.: 1369665-02-0
Formula: C₂₁H₂₁F₃IN₃O₂.1/2C₄H₄O₄
Molecular Weight:589.25

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Cobimetinib hemifumarate Chemical Structure

CAS No.: 1369665-02-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (63)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Cobimetinib hemifumarate is a novel selective MEK1 inhibitor, and the IC₅₀ value against MEK1 is 4.2 nM.

IC₅₀ & Target^[1]

MEK1

4.2 nM (IC₅₀)

All MEK Isoforms :

In Vitro

The EC₅₀ values of Cobimetinib (GDC-0973) for 888MEL and A2058 cells are 0.2 μM, 10 μM, respectivelly. Melanoma cells are treated with EC₅₀ concentration of MEK and PI3K inhibitors for 24 hours (888MEL: 0.05 μM GDC-0973, 2.5 μM GDC-0941; A2058: 2.5 μM GDC-0973, 2.5 μM GDC-0941)^[1]. Mitochondrial OXPHOS limits cell death induced by cobimetinib (100 nM) in melanoma with constitutive MAPK activation in A375 cells^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In the NCI-H2122 KRASG12C mutant non-small cell lung carcinoma (NSCLC) xenograft model, treatment with up to 5 mg/kg Cobimetinib (GDC-0973) lead to moderate TGI and at 10 mg/kg approaches tumor stasis^[1]. GDC-0973 and GDC-0941 are administered to A2058 tumor-bearing mice daily (QD) or every third day (Q3D) either as single agents or in combination. The population rate constants associated with tumor growth inhibition for GDC-0973 and GDC-0941 are 0.00102 and 0000651 μM^-1 h^-1, respectively^[2]. Following single doses of GDC-0973 (1, 3, or 10 mg/kg, p.o.) estimated in vivo IC₅₀ values of %pERK decrease based on tumor concentrations in xenograft mice are 0.78 (WM-266-4) and 0.52 μM (A375)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 1369665-02-0
Appearance Solid
Molecular Weight 589.25
Formula C₂₁H₂₁F₃IN₃O₂.1/2C₄H₄O₄
Color White to off-white
SMILES

OC1(CN(C(C2=C(NC3=C(F)C=C(I)C=C3)C(F)=C(F)C=C2)=O)C1)[C@H]4NCCCC4.O=C(/C=C/C(O)=O)O.[0.5]
Synonyms

GDC-0973 hemifumarate; XL-518 hemifumarate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (63)

All Apoptosis AnalysisFlow CytometryWBIn Vivo Efficacy StudyCell Proliferation/Viability AssayIHC

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Journal Impact Factor

Nat Nanotechnol

Therapeutically reprogrammed nutrient signalling enhances nanoparticulate albumin bound drug uptake and efficacy in KRAS-mutant cancer. [Abstract]

2021 Jul;16(7):830-839. PMID: 33958764
Bioact Mater

Modeling human hypertrophic scars with 3D preformed cellular aggregates bioprinting. [Abstract]

2021 Sep 8:10:247-254. PMID: 34901543
Cancer Res

Activity and Resistance of a Brain-Permeable Paradox Breaker BRAF Inhibitor in Melanoma Brain Metastasis. [Abstract]

2022 Jul 18;82(14):2552-2564. PMID: 35584009
Cancer Res

MEK Inhibition Remodels the Immune Landscape of Mutant KRAS Tumors to Overcome Resistance to PARP and Immune Checkpoint Inhibitors. [Abstract]

2021 May 15;81(10):2714-2729. PMID: 33589518
Nat Chem Biol

MEK interactions tune RAF kinase sensitivity to conformation-selective inhibition. [Abstract]

2026 May 12:10.1038/s41589-026-02212-2. PMID: 42120500
Sci Transl Med

A chimeric antigen receptor with antigen-independent OX40 signaling mediates potent antitumor activity. [Abstract]

2021 Jan 27;13(578):eaba7308. PMID: 33504651
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Cell Rep Med

CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]

2025 Apr 15;6(4):102053. PMID: 40187357
Blood Cancer J

Effective Menin inhibitor-based combinations against AML with MLL rearrangement or NPM1 mutation (NPM1c). [Abstract]

2022 Jan 11;12(1):5. PMID: 35017466

Cobimetinib hemifumarate purchased from MedChemExpress. Usage Cited in: Blood Cancer J. 2022 Jan 11;12(1):5. [Abstract]

OCI-AML3 cells were treated with the indicated concentrations of SNDX-50469, without or with 250 nM of MEK inhibitor Cobimetinib for 48 hours. Then, the % of annexin-V positive, apoptotic cells were determined by flow cytometry.

Cobimetinib hemifumarate purchased from MedChemExpress. Usage Cited in: Blood Cancer J. 2022 Jan 11;12(1):5. [Abstract]

OCI-AML3 cells were treated with the indicated concentration of SNDX-50469 for 48 hours, without or with 250 nM of MEK inhibitor Cobimetinib (added in the last 24 hours of treatment). Total cell lysates were prepared and immunoblot analyses were conducted.
Neuro Oncol

Preclinical assessment of MEK1/2 inhibitors for neurofibromatosis type 2-associated schwannomas reveals differences in efficacy and drug resistance development. [Abstract]

2019 Mar 18;21(4):486-497. PMID: 30615146
J Control Release

Cytotoxicity of PEGylated liposomes co-loaded with novel pro-apoptotic drug NCL-240 and the MEK inhibitor cobimetinib against colon carcinoma in vitro. [Abstract]

2015 Dec 28;220(Pt A):160-168. PMID: 26497930

Cobimetinib hemifumarate purchased from MedChemExpress. Usage Cited in: J Control Release. 2015 Dec 28;220(Pt A):160-168. [Abstract]

In vitro cytotoxicity analysis on HCT 116 cells showing enhanced cancer cell cytotoxicity of NCL and Cobimetinib (0.1-1 μM) combinations.
J Immunother Cancer

Tempered signal strength via low-dose MEK inhibition optimizes therapeutic performance of engineered T cells. [Abstract]

2025 Dec 1;13(12):e012800. PMID: 41330614

Cobimetinib hemifumarate purchased from MedChemExpress. Usage Cited in: J Immunother Cancer. 2025 Dec 1;13(12):e012800. [Abstract]

Representative flow cytometry plot of intracellular levels of phospho (p)-p42/44 (p-Erk1/2) on increasing doses of Cobimetinib (0-1 μM) after unspecific T cell activation via PMA/Ionomycin.

Cobimetinib hemifumarate purchased from MedChemExpress. Usage Cited in: J Immunother Cancer. 2025 Dec 1;13(12):e012800. [Abstract]

Cobimetinib (COB; 1 mg/kg; ip). Tumor area of tumor-bearing NSG mice in cm2 as measured by digital caliper after injection of TCR-T cells and COB.

Cobimetinib hemifumarate purchased from MedChemExpress. Usage Cited in: J Immunother Cancer. 2025 Dec 1;13(12):e012800. [Abstract]

Cobimetinib (COB; 1 mg/kg; ip). Immunohistochemistry anti-CD8-staining of one representative tumor for the PBS (left) versus COB-treated (right) group.
J Exp Med

Ferrous iron-activatable drug conjugate achieves potent MAPK blockade in KRAS-driven tumors. [Abstract]

2022 Apr 4;219(4):e20210739. PMID: 35262628
Mol Med

Activation of the MEK1-CHK2 axis in macrophages by Staphylococcus aureus promotes mitophagy, resulting in a reduction in bactericidal efficacy. [Abstract]

2025 May 29;31(1):211. PMID: 40437411
Clin Transl Med

Multi-omic profiling defines three distinct molecular subtypes of urothelial carcinoma with implications for precision therapy. [Abstract]

2026 Mar;16(3):e70638. PMID: 41804750
EMBO Mol Med

LIF, a mitogen for choroidal endothelial cells, protects the choriocapillaris: implications for prevention of geographic atrophy. [Abstract]

2022 Jan 11;14(1):e14511. PMID: 34779136
Cell Rep

Single-cell transcriptomics of NRAS-mutated melanoma transitioning to drug resistance reveals P2RX7 as an indicator of early drug response. [Abstract]

2023 Jun 27;42(7):112696. PMID: 37379213
Cell Rep

Kinetics of RTK activation determine ERK reactivation and resistance to dual BRAF/MEK inhibition in melanoma. [Abstract]

2023 May 29;42(6):112570. PMID: 37252843
Cell Syst

Large-scale control over collective cell migration using light-activated epidermal growth factor receptors. [Abstract]

2025 Mar 19;16(3):101203. PMID: 40037348
Cell Syst

Receptor-Driven ERK Pulses Reconfigure MAPK Signaling and Enable Persistence of Drug-Adapted BRAF-Mutant Melanoma Cells. [Abstract]

2020 Nov 18;11(5):478-494.e9. PMID: 33113355
Int J Oncol

Epigenetic inhibitors eliminate senescent melanoma BRAFV600E cells that survive long‑term BRAF inhibition. [Abstract]

2020 Jun;56(6):1429-1441. PMID: 32236593
Sci Data

High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]

2024 Sep 19;11(1):1024. PMID: 39300112
J Invest Dermatol

Combined Inhibition of MNK Signaling and BET Proteins Reveals TGM2 as a Novel Vulnerability in Melanoma. [Abstract]

2025 Apr;145(4):979-984.e5. PMID: 39357785
J Invest Dermatol

Combined Cyclin-Dependent Kinase Inhibition Overcomes MAPK/Extracellular Signal-Regulated Kinase Kinase Inhibitor Resistance in Plexiform Neurofibroma of Neurofibromatosis Type I. [Abstract]

2022 Mar;142(3 Pt A):613-623.e7. PMID: 34534577
Sci Signal

Activating mutations in MEK1 enhance homodimerization and promote tumorigenesis. [Abstract]

2018 Oct 30;11(554):eaar6795. PMID: 30377225
Biochem Pharmacol

MEK inhibitor induces cardiac complications by preventing ZMYND8-mediated ubiquitination and proteasomal degradation of HMGB1. [Abstract]

2026 Mar:245:117660. PMID: 41423035
Biochem Pharmacol

Celastrol synergizes with MEK1 inhibitor nedometinib to overcome resistance in bladder cancer via dual suppression of CDK1/CDC5L and feedback-activated Akt/STAT3. [Abstract]

2026 Mar:245:117629. PMID: 41386559
Cancer Metab

Long-acting Erwinia chrysanthemi, Pegcrisantaspase, induces alternate amino acid biosynthetic pathways in a preclinical model of pancreatic ductal adenocarcinoma. [Abstract]

2024 Jun 30;12(1):19. PMID: 38951899
Mol Cancer Res

TANKYRASE Inhibition Enhances the Antiproliferative Effect of PI3K and EGFR Inhibition, Mutually Affecting β-CATENIN and AKT Signaling in Colorectal Cancer. [Abstract]

2018 Mar;16(3):543-553. PMID: 29222171
Biomolecules

Allosteric Kinase Inhibitors Reshape MEK1 Kinase Activity Conformations in Cells and In Silico. [Abstract]

2021 Mar 30;11(4):518. PMID: 33808483
Mol Pharm

Molecular Interactions of Cobimetinib and Vemurafenib with Human Serum Albumin: a Comparative Biophysical and Computational Analysis. [Abstract]

2025 Aug 4;22(8):4969-4982. PMID: 40662409
Cancers (Basel)

In Vitro and In Vivo Drug-Response Profiling Using Patient-Derived High-Grade Glioma. [Abstract]

2023 Jun 22;15(13):3289. PMID: 37444398
Cancers (Basel)

Identification of New Vulnerabilities in Conjunctival Melanoma Using Image-Based High Content Drug Screening. [Abstract]

2022 Mar 19;14(6):1575. PMID: 35326726
Cancers (Basel)

MEK Inhibition Induces Canonical WNT Signaling through YAP in KRAS Mutated HCT-15 Cells, and a Cancer Preventive FOXO3/FOXM1 Ratio in Combination with TNKS Inhibition. [Abstract]

2019 Feb 1;11(2):164. PMID: 30717152
Mol Immunol

Rosmarinic acid activates the Ras/Raf/MEK/ERK signaling pathway to regulate CD8+ T cells and autophagy to clear Chlamydia trachomatis in reproductive tract-infected mice. [Abstract]

2024 Jul:171:105-114. PMID: 38820902
Exp Cell Res

Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]

2020 Aug 1;393(1):112054. PMID: 32376287
Nucl Med Biol

A novel synergistic drug combination of a mitogen-activated extracellular signal-regulated kinase inhibitor with [177Lu]Lu-rhPSMA-10.1 for prostate cancer treatment: Results of a preclinical evaluation. [Abstract]

2025 Jun 8:146-147:109042. PMID: 40517460
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
bioRxiv

2026 Mar 13.
Charles University

2026.
bioRxiv

2026 Feb 23.
Technical University of Dresden

2025.
University of Kansas

2025.
Princeton University

2025.
Patent

US20250099450A1.
bioRxiv

Capacity for compensatory cyclin D2 response confers trametinib resistance in canine mucosal melanoma. [Abstract]

2025 Apr 26:2025.04.24.650512. PMID: 40568110
Research Square Preprint

2024 Oct 10.
Research Square Preprint

2024 Nov 06.
Patent

WO2020142349A1.
bioRxiv

2024 September 19.
bioRxiv

Large-scale control over collective cell migration using light-controlled epidermal growth factor receptors. [Abstract]

2024 May 31:2024.05.30.596676. PMID: 38853934
Research Square Preprint

2022 Jul.
Elife

RNF43 inhibits WNT5A-driven signaling and suppresses melanoma invasion and resistance to the targeted therapy. [Abstract]

2021 Oct 27;10:e65759. PMID: 34702444
Oncotarget

MEK is a promising target in the basal subtype of bladder cancer. [Abstract]

2020 Nov 3;11(44):3921-3932. PMID: 33216841
SSRN

2020 May.
ACS Comb Sci

Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]

2019 Dec 9;21(12):805-816. PMID: 31689077
bioRxiv

2019 Sep.
Methods Mol Biol

Methods for High-throughput Drug Combination Screening and Synergy Scoring. [Abstract]

2018:1711:351-398. PMID: 29344898
Patent

US20170326205A1.
Patent

US9724393B2.
Oslo University

2017 May.
Patent

US20170020964A1.
Northeastern University

2016 Jan.

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (84.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6971 mL

8.4854 mL

16.9707 mL

5 mM

0.3394 mL

1.6971 mL

3.3941 mL

10 mM

0.1697 mL

0.8485 mL

1.6971 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Dilution Calculator

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline