1. MAPK/ERK Pathway
  2. MEK
  3. Cobimetinib

Cobimetinib (Synonyms: GDC-0973; XL518)

Cat. No.: HY-13064 Purity: 99.70%
Handling Instructions

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.

Cobimetinib Chemical Structure

Cobimetinib Chemical Structure

CAS No. : 934660-93-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 112 In-stock
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
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10 mg USD 120 In-stock
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50 mg USD 396 In-stock
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100 mg USD 576 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of Cobimetinib:

Top Publications Citing Use of Products

    Cobimetinib purchased from MCE. Usage Cited in: J Control Release. 2015 Oct 21;220(Pt A):160-168.

    In vitro cytotoxicity analysis on HCT 116 cells showing enhanced cancer cell cytotoxicity of NCL and Cobimetinib combinations

    Cobimetinib purchased from MCE. 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 purchased from MCE. Usage Cited in: Sci Signal. 2018 Oct 30;11(554). pii: eaar6795. 

    MEK1 mutants with in-frame deletions of the β3-αC loop exhibit differential resistance to MEK inhibitors (Trametinib, GDC0623, cobimetinib, AZD6244, and binimentinib).

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    • Biological Activity

    • Protocol

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    • References

    • Customer Review

    Description

    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)

    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].

    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].

    Clinical Trial
    Molecular Weight

    531.31

    Formula

    C₂₁H₂₁F₃IN₃O₂

    CAS No.

    934660-93-2

    SMILES

    OC1([[email protected]]2NCCCC2)CN(C1)C(C3=C(C(F)=C(C=C3)F)NC4=C(C=C(C=C4)I)F)=O

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (188.21 mM)

    *"≥" means soluble, but saturation unknown.

    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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    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

    Purity: 99.70%

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    Product Name:
    Cobimetinib
    Cat. No.:
    HY-13064
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