Art. -Nr.: HY-13064

Cobimetinib

(Synonyms: GDC-0973; XL518)

63 Cited Publications

Kundenbewertung

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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.81%
CAS. Nr.: 934660-93-2
Formel: C₂₁H₂₁F₃IN₃O₂
Molecular Weight:531.31

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Cobimetinib Chemical Structure

CAS. Nr.: 934660-93-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (63)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC₅₀ of 4.2 nM for MEK1.

IC₅₀ & Target^[1]

MEK1

4.2 nM (IC₅₀)

Alle MEK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	5 nM Compound: Cobimetinib	Antiproliferative activity against human A375 cells assessed as reduction in cell viability Antiproliferative activity against human A375 cells assessed as reduction in cell viability	[PMID: 31804822]
COLO 205	IC₅₀	1.8 nM Compound: GDC-0973	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	[PMID: 22315332]
COLO 205	IC₅₀	8 nM Compound: GDC-0973	Antiproliferative activity against human COLO205 cells expressing B-raf V600E mutant Antiproliferative activity against human COLO205 cells expressing B-raf V600E mutant	[PMID: 22315332]
IMR-32	IC₅₀	0.07 μM Compound: 46	Antiproliferative activity against human IMR-32 cells assessed as cell growth inhibition Antiproliferative activity against human IMR-32 cells assessed as cell growth inhibition	[PMID: 32937281]

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 934660-93-2
Appearance Solid
Molecular Weight 531.31
Formel C₂₁H₂₁F₃IN₃O₂
Color White to off-white
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
Synonyms

GDC-0973; XL518
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

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 2:102053. 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 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.
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 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.
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.
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]

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
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

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.

Lösungsmittel & Löslichkeit

In Vitro:

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)

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

1.8821 mL

9.4107 mL

18.8214 mL

5 mM

0.3764 mL

1.8821 mL

3.7643 mL

10 mM

0.1882 mL

0.9411 mL

1.8821 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, 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Animal Administration^[3]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
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- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Cobimetinib

63 Cited Publications

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Cobimetinib

Apoptosis Compound Library

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Publications Citing Use of MedChemExpress (MCE) Cobimetinib

Alle MEK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

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