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Cobimetinib
$96 – $576
Products Details
Product Description
– Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.
Web ID
– HY-13064
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C21H21F3IN3O2
Citations
– ACS Comb Sci. 2019 Dec 9;21(12):805-816.|Bioact Mater. 8 September 2021.|Biomolecules. 2021 Mar 30;11(4):518.|bioRxiv. 2019 Sep.|Blood Cancer J. 2022 Jan 11;12(1):5.|Cancer Res. 2021 Feb 15;canres.2370.2020.|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. 2023 Jun 27;42(7):112696.|Cell Rep. 2023 May 29;42(6):112570.|Cell Syst. 2020 Nov 18;11(5):478-494.e9.|Department of Microbiology. Oslo University. 2017 May.|Elife. 2021 Oct 27;10:e65759.|EMBO Mol Med. 2021 Nov 15;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. 2021 Sep 14;S0022-202X(21)01672-9.|Methods Mol Biol. 2018;1711:351-398.|Mol Cancer Res. 2018 Mar;16(3):543-553.|Nat Nanotechnol. 2021 Jul;16(7):830-839.|Neuro Oncol. 2019 Mar 18;21(4):486-497. |Oncotarget. 2020 Nov 3;11(44):3921-3932.|Patent. US20170020964A1.|Patent. US20170326205A1.|Patent. US9724393B2.|Research Square Preprint. 2022 Jul.|School of Health Sciences. Northeastern University. 2016 Jan.|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.|Cancer Res. 2022 May 18;canres.4152.2021.
References
– [1]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.|[2]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.|[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.
CAS Number
– 934660-93-2
Molecular Weight
– 531.31
Compound Purity
– 99.73
SMILES
– OC1([C@H]2NCCCC2)CN(C1)C(C3=C(C(F)=C(C=C3)F)NC4=C(C=C(C=C4)I)F)=O
Clinical Information
– Launched
Research Area
– Cancer
Solubility
– DMSO : 50 mg/mL (ultrasonic;warming;heat to 60°C)|H2O : 1 mg/mL (ultrasonic;warming;heat to 60°C)
Target
– Apoptosis;MEK
Isoform
– MEK1
Pathway
– Apoptosis;MAPK/ERK Pathway
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
