Cobimetinib (Synonyms: GDC-0973; XL518)

Name: Cobimetinib
Brand: MedChemExpress
SKU: HY-13064
Rating: 5.0 (62 reviews)

Cat. No.: HY-13064 Purity: 99.81%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No. : 934660-93-2

사이즈	재고	수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

or 대량구매 문의

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 62 publication(s) in Google Scholar

Other Forms of Cobimetinib:

62 Publications Citing Use of MCE Cobimetinib

Apoptosis Analysis

Flow Cytometry

In Vivo Efficacy Study

Cell Proliferation/Viability Assay

IHC

: 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.

: 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.

: 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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MEK1 MEK2 MEK5 MEK MAP2K4/MEK4 MAP2K7/MEK7

Biological Activity
Protocol
순도&문서
References
고객리뷰

제품 설명

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)

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

분자량

531.31

화학식

C₂₁H₂₁F₃IN₃O₂

CAS No.

934660-93-2

Appearance

Solid

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

선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

몰농도 계산기
농도 희석 계산기

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

순도&문서

Purity: 99.81%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (249 KB) HNMR (271 KB) RP-HPLC (270 KB) LCMS (96 KB) Elemental Analysis Report (106 KB)

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]

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.

MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.

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

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

Cobimetinib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cobimetinib934660-93-2GDC-0973 XL518GDC0973GDC 0973XL518XL 518XL-518MEKApoptosisMitogen-activated protein kinase kinaseMAPKKMAP2KInhibitorinhibitorinhibit

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Cobimetinib (Synonyms: GDC-0973; XL518)

고객리뷰

Other Forms of Cobimetinib:

Cobimetinib Related Antibodies

62 Publications Citing Use of MCE Cobimetinib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All MEK Isoform Specific Products:

Biological Activity

Protocol

순도&문서

References

고객리뷰

Cobimetinib Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

Cobimetinib Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report