Cobimetinib
Based on 63 publication(s) in Google Scholar
Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.
For research use only. We do not sell to patients.
- Purity: 99.81%
- CAS No.: 934660-93-2
- Formula: C21H21F3IN3O2
- Molecular Weight:531.31
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) Cobimetinib
More- Nat Nanotechnol. 2021 Jul;16(7):830-839. [Abstract]
- Bioact Mater. 2021 Sep 8:10:247-254. [Abstract]
- Cancer Res. 2022 Jul 18;82(14):2552-2564. [Abstract]
- Cancer Res. 2021 May 15;81(10):2714-2729. [Abstract]
- Sci Transl Med. 2021 Jan 27;13(578):eaba7308. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Nat Chem Biol. 2026 May 12:10.1038/s41589-026-02212-2. [Abstract]
- Neuro Oncol. 2019 Mar 18;21(4):486-497. [Abstract]
- Blood Cancer J. 2022 Jan 11;12(1):5. [Abstract]
- J Control Release. 2015 Oct 21;220(Pt A):160-168. [Abstract]
- J Immunother Cancer. 2025 Dec 1;13(12):e012800. [Abstract]
- Cell Rep Med. 2025 Apr 2:102053. [Abstract]
- J Exp Med. 2022 Apr 4;219(4):e20210739. [Abstract]
- EMBO Mol Med. 2022 Jan 11;14(1):e14511. [Abstract]
- Cell Syst. 2025 Mar 19;16(3):101203. [Abstract]
- Cell Syst. 2020 Nov 18;11(5):478-494.e9. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- Cell Rep. 2023 Jun 27;42(7):112696. [Abstract]
- Cell Rep. 2023 May 29;42(6):112570. [Abstract]
- Clin Transl Med. 2026 Mar;16(3):e70638. [Abstract]
- Sci Signal. 2018 Oct 30;11(554):eaar6795. [Abstract]
- Mol Med. 2025 May 29;31(1):211. [Abstract]
- Elife. 2021 Oct 27;10:e65759. [Abstract]
- J Invest Dermatol. 2025 Apr;145(4):979-984.e5. [Abstract]
- J Invest Dermatol. 2022 Mar;142(3 Pt A):613-623.e7. [Abstract]
- Biochem Pharmacol. 2025 Dec 19:245:117660. [Abstract]
- Biochem Pharmacol. 2025 Dec 10:245:117629. [Abstract]
- Cancer Metab. 2024 Jun 30;12(1):19. [Abstract]
- Int J Oncol. 2020 Jun;56(6):1429-1441. [Abstract]
- Biomolecules. 2021 Mar 30;11(4):518. [Abstract]
- Mol Cancer Res. 2018 Mar;16(3):543-553. [Abstract]
- Mol Pharm. 2025 Aug 4;22(8):4969-4982. [Abstract]
- Cancers (Basel). 2023 Jun 22;15(13):3289. [Abstract]
- Cancers (Basel). 2022 Mar 19;14(6):1575. [Abstract]
- Cancers. 2019 Feb 1;11(2):164. [Abstract]
- Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
- Nucl Med Biol. 2025 Jun 8:146-147:109042. [Abstract]
- Mol Immunol. 2024 Jul:171:105-114. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- 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. 2025 Apr 26:2025.04.24.650512. [Abstract]
- Research Square Preprint. 2024 Oct 10.
- Research Square Preprint. 2024 Nov 06.
- Patent. WO2020142349A1.
- bioRxiv. 2024 September 19.
- bioRxiv. 2024 May 31:2024.05.30.596676. [Abstract]
- Research Square Preprint. 2022 Jul.
- Oncotarget. 2020 Nov 3;11(44):3921-3932. [Abstract]
- SSRN. 2020 May.
- ACS Comb Sci. 2019 Dec 9;21(12):805-816. [Abstract]
- bioRxiv. 2019 Sep.
- Methods Mol Biol. 2018:1711:351-398. [Abstract]
- Patent. US20170326205A1.
- Patent. US9724393B2.
- Oslo University. 2017 May.
- Patent. US20170020964A1.
- Northeastern University. 2016 Jan.
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Flow Cytometry
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In Vivo Efficacy Study
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IHC
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Apoptosis Analysis
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WB
All MEK Isoforms
More
Biological Activity
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MEK1 4.2 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
5 nM
Compound: Cobimetinib
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Antiproliferative activity against human A375 cells assessed as reduction in cell viability
Antiproliferative activity against human A375 cells assessed as reduction in cell viability
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[PMID: 31804822] |
| COLO 205 | IC50 |
1.8 nM
Compound: GDC-0973
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Inhibition of B-raf V600E mutant in human COLO205 cells assessed as reduction of ERK1/ERK2 phosphorylation
Inhibition of B-raf V600E mutant in human COLO205 cells assessed as reduction of ERK1/ERK2 phosphorylation
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[PMID: 22315332] |
| COLO 205 | IC50 |
8 nM
Compound: GDC-0973
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Antiproliferative activity against human COLO205 cells expressing B-raf V600E mutant
Antiproliferative activity against human COLO205 cells expressing B-raf V600E mutant
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[PMID: 22315332] |
| IMR-32 | IC50 |
0.07 μM
Compound: 46
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Antiproliferative activity against human IMR-32 cells assessed as cell growth inhibition
Antiproliferative activity against human IMR-32 cells assessed as cell growth inhibition
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[PMID: 32937281] |
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 934660-93-2
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Appearance Solid
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Molecular Weight 531.31
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Formula C21H21F3IN3O2
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Color White to off-white
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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
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Synonyms
GDC-0973; XL518
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (63)
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Journal Impact Factor
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Most Recent
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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
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 -
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 -
Nat Chem Biol
2026 May 12:10.1038/s41589-026-02212-2. PMID: 42120500 -
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 -
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 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 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.
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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 Oct 21;220(Pt A):160-168. PMID: 26497930
Cobimetinib purchased from MedChemExpress. Usage Cited in: J Control Release. 2015 Oct 21;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.
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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 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 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 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.
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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 2:102053. PMID: 40187357 -
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 -
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 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 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
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 -
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 -
Sci Signal
2018 Oct 30;11(554):eaar6795. PMID: 30377225 -
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 -
Elife
RNF43 inhibits WNT5A-driven signaling and suppresses melanoma invasion and resistance to the targeted therapy. [Abstract]2021 Oct 27;10:e65759. PMID: 34702444 -
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 -
Biochem Pharmacol
MEK inhibitor induces cardiac complications by preventing ZMYND8-mediated ubiquitination and proteasomal degradation of HMGB1. [Abstract]2025 Dec 19:245:117660. 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]2025 Dec 10:245:117629. 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 -
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 -
Biomolecules
Allosteric Kinase Inhibitors Reshape MEK1 Kinase Activity Conformations in Cells and In Silico. [Abstract]2021 Mar 30;11(4):518. PMID: 33808483 -
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 -
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)
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
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 -
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 -
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 -
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 -
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bioRxiv
Capacity for compensatory cyclin D2 response confers trametinib resistance in canine mucosal melanoma. [Abstract]2025 Apr 26:2025.04.24.650512. PMID: 40568110 -
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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 -
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Oncotarget
2020 Nov 3;11(44):3921-3932. PMID: 33216841 -
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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 -
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Methods Mol Biol
2018:1711:351-398. PMID: 29344898 -
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Solvent & Solubility
DMSO : 50 mg/mL (94.11 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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-
-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
5 million WM-266-4 melanoma cells are resuspended in Hank balanced salt solution and implanted intradermally into the hind flank of female NCR nude mice. On days 11 or 13 after the implantation, xenograft mice with tumor volumes of approximately 100 to 120 mm3 are randomLy assigned to 8 groups (n=27 per group), 4 single dose groups and 4 multiple dose groups. One day after randomization and group assignment, mice in the single dose groups are given a single oral dose of vehicle (water for injection USP), 1, 3, or 10 mg/kg of Cobimetinib (GDC-0973, expressed as free base equivalents). Mice in the multiple dose groups are given daily oral doses of vehicle (water for injection USP), 1, 3, or 10 mg/kg of GDC-0973 for 14 days. Plasma and tumor samples (n=3 per time point) are collected from euthanized mice predose and at 2, 4, 8, 16, 24, 72, 120, and 168 hours postdose on day 1 (single dose groups) or day 14 (multiple dose groups). Samples are stored at −80°C until analysis. GDC-0973 concentrations in plasma and tumor lysates are determined using liquid chromatography/tandem mass spectrometry (LC/MS-MS). The dynamic range of the assay is 0.004 to 35 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8821 mL | 9.4107 mL | 18.8214 mL | 47.0535 mL |
| 5 mM | 0.3764 mL | 1.8821 mL | 3.7643 mL | 9.4107 mL | |
| 10 mM | 0.1882 mL | 0.9411 mL | 1.8821 mL | 4.7054 mL | |
| 15 mM | 0.1255 mL | 0.6274 mL | 1.2548 mL | 3.1369 mL | |
| 20 mM | 0.0941 mL | 0.4705 mL | 0.9411 mL | 2.3527 mL | |
| 25 mM | 0.0753 mL | 0.3764 mL | 0.7529 mL | 1.8821 mL | |
| 30 mM | 0.0627 mL | 0.3137 mL | 0.6274 mL | 1.5685 mL | |
| 40 mM | 0.0471 mL | 0.2353 mL | 0.4705 mL | 1.1763 mL | |
| 50 mM | 0.0376 mL | 0.1882 mL | 0.3764 mL | 0.9411 mL | |
| 60 mM | 0.0314 mL | 0.1568 mL | 0.3137 mL | 0.7842 mL | |
| 80 mM | 0.0235 mL | 0.1176 mL | 0.2353 mL | 0.5882 mL |