2. MAPK/ERK Pathway Apoptosis
  3. MEK Apoptosis
  4. Cobimetinib hemifumarate

Cobimetinib hemifumarate  (Synonyms: GDC-0973 hemifumarate; XL-518 hemifumarate)

Cat. No.: HY-13064A Purity: 99.73%
COA Handling Instructions

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Cobimetinib hemifumarate is a novel selective MEK1 inhibitor, and the IC50 value against MEK1 is 4.2 nM.

For research use only. We do not sell to patients.

Cobimetinib hemifumarate Chemical Structure

Cobimetinib hemifumarate Chemical Structure

CAS No. : 1369665-02-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 124 In-stock
Solution
10 mM * 1 mL in DMSO USD 124 In-stock
Solid
5 mg USD 96 In-stock
10 mg USD 120 In-stock
50 mg USD 396 In-stock
100 mg USD 576 In-stock
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Customer Review

Based on 43 publication(s) in Google Scholar

Other Forms of Cobimetinib hemifumarate:

Cobimetinib hemifumarate Related Antibodies

Top Publications Citing Use of Products

41 Publications Citing Use of MCE Cobimetinib hemifumarate

Proliferation Assay
WB

    Cobimetinib hemifumarate purchased from MedChemExpress. Usage Cited in: Department of Microbiology. Oslo University. 2017 May.

    Western blot protein analysis detecting levels of Non N-terminal phosphorylated (active) β-catenin (ABC) protein levels and total amount of β-catenin in both COLO 320DM and HCT-15 cells upon 0,04% DMSO, 1 µM G007-LK, 3 µM GDC-0973 and 1µM G007-LK + 3 µM GDC-0973 treatment.

    Cobimetinib hemifumarate 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 combinations

    View All MEK Isoform Specific Products:

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    MEK1 MEK2 MEK5 MEK

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Cobimetinib hemifumarate is a novel selective MEK1 inhibitor, and the IC50 value against MEK1 is 4.2 nM.

    IC50 & Target[1]

    MEK1

    4.2 nM (IC50)

    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.

    Cobimetinib hemifumarate Related Antibodies
    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
    Molecular Weight

    589.25

    Formula

    C21H21F3IN3O2.1/2C4H4O4
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    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.[0.5]
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (84.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.6971 mL 8.4854 mL 16.9707 mL
    5 mM 0.3394 mL 1.6971 mL 3.3941 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    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 (4.24 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 (4.24 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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.
    Purity & Documentation

    Purity: 99.73%

    COA (254 KB) RP-HPLC (201 KB)

    Handling Instructions (2659 KB)
    References
    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 has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.6971 mL 8.4854 mL 16.9707 mL 42.4268 mL
    5 mM 0.3394 mL 1.6971 mL 3.3941 mL 8.4854 mL
    10 mM 0.1697 mL 0.8485 mL 1.6971 mL 4.2427 mL
    15 mM 0.1131 mL 0.5657 mL 1.1314 mL 2.8285 mL
    20 mM 0.0849 mL 0.4243 mL 0.8485 mL 2.1213 mL
    25 mM 0.0679 mL 0.3394 mL 0.6788 mL 1.6971 mL
    30 mM 0.0566 mL 0.2828 mL 0.5657 mL 1.4142 mL
    40 mM 0.0424 mL 0.2121 mL 0.4243 mL 1.0607 mL
    50 mM 0.0339 mL 0.1697 mL 0.3394 mL 0.8485 mL
    60 mM 0.0283 mL 0.1414 mL 0.2828 mL 0.7071 mL
    80 mM 0.0212 mL 0.1061 mL 0.2121 mL 0.5303 mL
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    Cobimetinib hemifumarate 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:

    Cobimetinib hemifumarate1369665-02-0GDC-0973 hemifumarateXL-518 hemifumarateMEKApoptosisMitogen-activated protein kinase kinaseMAPKKMAP2KInhibitorinhibitorinhibit

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