Cobimetinib (hemifumarate)
Cobimetinib hemifumarate is a novel selective MEK1 inhibitor, and the IC50 value against MEK1 is 4.2 nM.
Product Specifications
CAS Number
[1369665-02-0]
Product Name Alternative
GDC-0973 (hemifumarate) ; XL-518 (hemifumarate)
UNSPSC
12352005
Target
Apoptosis; MEK
Type
Reference compound
Related Pathways
Apoptosis; MAPK/ERK Pathway
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/Cobimetinib_hemifumarate.html
Purity
99.68
Solubility
DMSO : 50 mg/mL (ultrasonic)
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
Molecular Formula
C21H21F3IN3O2.1/2C4H4O4
Molecular Weight
589.25
References & Citations
[1]Hoeflich KP, et al. Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition. Cancer Res. 2012 Jan 1;72 (1) :210-9.|[2]Choo EF, et al. PK-PD modeling of combination efficacy effect from administration of the MEK inhibitor GDC-0973 and PI3K inhibitor GDC-0941 in A2058 xenografts. Cancer Chemother Pharmacol. 2013 Jan;71 (1) :133-43.|[3]Wong H, et al. Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor. Clin Cancer Res. 2012 Jun 1;18 (11) :3090-9.|[4]Corazao-Rozas P, et al. Mitochondrial oxidative phosphorylation controls cancer cell's life and death decisions upon exposure to MAPK inhibitors. Oncotarget. 2016 Feb 29. doi: 10.18632/oncotarget.7790.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
MEK1
Citation 01
Cancer Res. 2022 Jul 18;82 (14) :2552-2564.|ACS Comb Sci. 2019 Dec 9;21 (12) :805-816.|Bioact Mater. 2021 Sep 8:10:247-254.|Biomolecules. 2021 Mar 30;11 (4) :518.|bioRxiv. 2019 Sep.|bioRxiv. 2024 May 31:2024.05.30.596676.|bioRxiv. 2024 September 19.|bioRxiv. 2025 Apr 26:2025.04.24.650512.|Blood Cancer J. 2022 Jan 11;12 (1) :5.|Cancer Metab. 2024 Jun 30;12 (1) :19.|Cancer Res. 2021 May 15;81 (10) :2714-2729.|Cancers (Basel) . 2022 Mar 19;14 (6) :1575.|Cancers (Basel) . 2023 Jun 22;15 (13) :3289.|Cancers. 2019 Feb 1;11 (2) :164.|Cell Rep Med. 2025 Apr 2:102053.|Cell Rep. 2023 Jun 27;42 (7) :112696.|Cell Rep. 2023 May 29;42 (6) :112570.|Cell Syst. 2020 Nov 18;11 (5) :478-494.e9.|Cell Syst. 2025 Mar 19;16 (3) :101203.|Department of Microbiology. Oslo University. 2017 May.|Elife. 2021 Oct 27;10:e65759.|EMBO Mol Med. 2022 Jan 11;14 (1) :e14511.|Exp Cell Res. 2020 Aug 1;393 (1) :112054.|Int J Oncol. 2020 Jun;56 (6) :1429-1441.|J Control Release. 2015 Oct 21;220 (Pt A) :160-168. |J Exp Med. 2022 Apr 4;219 (4) :e20210739.|J Invest Dermatol. 2022 Mar;142 (3 Pt A) :613-623.e7.|J Invest Dermatol. 2025 Apr;145 (4) :979-984.e5.|Methods Mol Biol. 2018:1711:351-398.|Mol Cancer Res. 2018 Mar;16 (3) :543-553.|Mol Immunol. 2024 Jul:171:105-114.|Mol Med. 2025 May 29;31 (1) :211.|Mol Pharm. 2025 Aug 4;22 (8) :4969-4982.|Nat Nanotechnol. 2021 Jul;16 (7) :830-839.|Neuro Oncol. 2019 Mar 18;21 (4) :486-497. |Nucl Med Biol. 2025 Jun 8:146-147:109042.|Oncotarget. 2020 Nov 3;11 (44) :3921-3932.|Patent. US20170020964A1.|Patent. US20170326205A1.|Patent. US20250099450A1.|Patent. US9724393B2.|Patent. WO2020142349A1.|PLoS One. 2024 Nov 1;19 (11) :e0308647.|Princeton University. 2025.|Research Square Preprint. 2022 Jul.|Research Square Preprint. 2024 Nov 06.|Research Square Preprint. 2024 Oct 10.|School of Health Sciences. Northeastern University. 2016 Jan.|Sci Data. 2024 Sep 19;11 (1) :1024.|Sci Signal. 2018 Oct 30;11 (554) :eaar6795.|Sci Transl Med. 2018 Jul 18;10 (450) :eaaq1093.|Sci Transl Med. 2021 Jan 27;13 (578) :eaba7308.|SSRN. 2020 May.|University of Kansas. 2025.
Available Sizes
Curated Selection
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