1. MAPK/ERK Pathway
    Stem Cell/Wnt
  2. ERK

GDC-0994 (Synonyms: Ravoxertinib)

Cat. No.: HY-15947 Purity: 99.79%
Handling Instructions

GDC-0994 is an orally bioavailable inhibitor selective for ERK kinase activity with IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.

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

GDC-0994 Chemical Structure

GDC-0994 Chemical Structure

CAS No. : 1453848-26-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
50 mg USD 360 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

Other Forms of GDC-0994:

    GDC-0994 purchased from MCE. Usage Cited in: Cell. 2018 Sep 20;175(1):186-199.e19.

    Cells are treated with EPZ-6438 (1 μM) or GSK126 (1 μM) for 6 days. Protein levels are analyzed by immunoblotting. Cells are treated with EPZ-6438 (1 μM), JQ1 (0.25 μM) alone or combination for 6 days. Protein levels are analyzed by immunoblotting.

    View All ERK Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    GDC-0994 is an orally bioavailable inhibitor selective for ERK kinase activity with IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.

    IC50 & Target[1]

    ERK2

    3.1 nM (IC50)

    ERK1

    6.1 nM (IC50)

    p-RSK

    12 nM (IC50)

    In Vitro

    GDC-0994 also inhibits p90RSK with IC50 of 12 nM[1]. GDC-0994 is highly selective for ERK1 and ERK2, with biochemical potency of 1.1 nM and 0.3 nM, respectively[2].

    In Vivo

    In CD-1 mice, a 10 mg/kg oral dose of GDC-0994 is sufficient to achieve the desired target coverage for at least 8 h[1]. Daily, oral dosing of GDC-0994 results in significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice[2].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 35 mg/mL (79.39 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2683 mL 11.3415 mL 22.6829 mL
    5 mM 0.4537 mL 2.2683 mL 4.5366 mL
    10 mM 0.2268 mL 1.1341 mL 2.2683 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      GDC-0994 is prepared in vehicle (0.5% CMCNa+0.1% Tween80+ddH2O)[3].

    References
    Animal Administration
    [1]

    Mice[1]
    PK/PD data for GDC-0994 in the HCT116 mouse xenograft model. HCT116 tumors are established in nude mice to a tumor volume of 400−600 mm3. Mice are treated with a single oral dose of 22 at 15, 30, or 100 mg/kg versus vehicle control alone (40% PEG400/60% (10% HPβCD)) follow by tumor and plasma collection at 2, 8, 16, and 24 h postdose. Tumor levels of phosphorylated p90RSK (pRSK) relative total p90RSK (tRSK) are measured by quantitative Western blot and are normalized to vehicle control at 2 h postdose (set to 100%). Plasma and tumor concentrations are measured by LC−MS.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    440.86

    Formula

    C₂₁H₁₈ClFN₆O₂

    CAS No.

    1453848-26-4

    SMILES

    O=C1C=C(C2=NC(NC3=CC=NN3C)=NC=C2)C=CN1[[email protected]@H](C4=CC=C(Cl)C(F)=C4)CO

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.79%

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number *

     

    Organization name *

    Country or Region *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    GDC-0994
    Cat. No.:
    HY-15947
    Quantity:

    GDC-0994

    Cat. No.: HY-15947