2. MAPK/ERK Pathway Stem Cell/Wnt
  3. ERK
  4. Ravoxertinib

Ravoxertinib (GDC-0994) is an orally active ERK kinase inhibitor with an IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.

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

CAS No. : 1453848-26-4

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Customer Review

Based on 51 publication(s) in Google Scholar

Other Forms of Ravoxertinib:

Ravoxertinib Related Antibodies

Top Publications Citing Use of Products

51 Publications Citing Use of MCE Ravoxertinib

RT-PCR
Cell Proliferation/Viability Assay
IP

    Ravoxertinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2026 Jan 21;17(1):1902.  [Abstract]

    U87, U251, and H1299 cells, with or without EGFR R252C mutation were treated with or without 5 μM Ravoxertinib. Cell proliferation was assessed at day 7. Relative proliferation was calculated using vehicle-treated EGFR WT cells as the control.

    Ravoxertinib purchased from MedChemExpress. Usage Cited in: Nature. 2025 Jan;637(8046):726-735.  [Abstract]

    Investigation of the signalling axis regulating LIF expression upon PDGF stimulation. Cells were treated with ERK inhibitor ravoxertinib (10 μM) for 24 h before cell lysis for total RNA extraction and measurement of LIF mRNA levels by real-time qPCR.

    Ravoxertinib purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2023 Feb;20(2):175-188.  [Abstract]

    Effects of kinase inhibitors on ISO-triggered inhibition of SeV-induced transcription of the IFNB1 gene. THP1 cells were treated with the ERK inhibitor GDC-0994 (1 μM) for 1 h and then were treated with ISO (10 μM) and infected with SeV (MOI = 1). Six hours later, a qPCR analysis to determine the mRNA levels of the IFNB1 gene was performed. The results are shown as the inhibition rate (%).

    Ravoxertinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Sep 30;14(1):6117.  [Abstract]

    HCT116 cells were pretreated with PPP (1 μM), ARQ-092 (2 μM) and GDC-0994 (Ravoxertinib, 10 μM) for 1 h before being cultured under hypoxia for 12 h.

    Ravoxertinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2023 Jul 13;42(1):166.  [Abstract]

    The effect of NF-κB, ERK, JNK and p38 inhibitors on IL-1β-induced Saa3 expression in vivo. One hour after intravenous administration of Ravoxertinib, IL-1β (20 ng in 100 ul saline) were i.v. administrated into the mice. Six hours later, lung Saa3 expression was detected by qPCR.

    Ravoxertinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2023 Jul 13;42(1):166.  [Abstract]

    The effect of NF-κB, ERK, JNK and p38 inhibitors on IL-1β-induced Saa3 expression in MLE-12 cells. MLE-12 cells were pre-treated with Ravoxertinib for 1 h, then stimulated with IL-1β (10 ng/ml) for 6 h. Saa3 expression was detected by qPCR.

    View All ERK Isoform Specific Products:

    View All Isoforms
    ERK ERK1 ERK2 ERK5 ERK8

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Ravoxertinib (GDC-0994) is an orally active ERK kinase inhibitor with an 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)

    Cellular Effect
    Cell Line Type Value Description References
    HepG2 IC50
    12 nM
    Compound: 22; GDC-0994
    Inhibition of ERK in PMA-stimulated human HepG2 cells assessed as inhibition of p90RSK serine-380 phosphorylation
    Inhibition of ERK in PMA-stimulated human HepG2 cells assessed as inhibition of p90RSK serine-380 phosphorylation
    		[PMID: 27227380]
    In Vitro

    Ravoxertinib (GDC-0994) also inhibits p90RSK with an IC50 of 12 nM[1].
    Ravoxertinib (GDC-0994) is highly selective for ERK1 and ERK2, with biochemical potency of 1.1 nM and 0.3 nM, respectively[2].
    Ravoxertinib (GDC0994; 50 nM, 0.5 μM, and 5 μM; 48 hours) decreases the viability of lung adenocarcinoma cell lines (A549, HCC827, HCC4006)[3].

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

    Ravoxertinib Related Antibodies
    In Vivo

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

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    440.86

    Formula

    C21H18ClFN6O2
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 35 mg/mL (79.39 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" 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
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • 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)

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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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.5 mg/mL (5.67 mM); Clear solution

    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1.67 mg/mL (3.79 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  30% PEG300    70% (10% HP-β-CD in Saline)

      Solubility: 5 mg/mL (11.34 mM); Clear solution; Need ultrasonic

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

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    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.
    Purity & Documentation

    Purity: 99.84%

    SDS (393 KB)

    COA (252 KB) HNMR (276 KB) LCMS (95 KB)

    Handling Instructions (2659 KB)
    References
    Animal Administration
    [1]

    Mice[1]
    PK/PD data for Ravoxertinib (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

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2683 mL 11.3415 mL 22.6829 mL 56.7073 mL
    5 mM 0.4537 mL 2.2683 mL 4.5366 mL 11.3415 mL
    10 mM 0.2268 mL 1.1341 mL 2.2683 mL 5.6707 mL
    15 mM 0.1512 mL 0.7561 mL 1.5122 mL 3.7805 mL
    20 mM 0.1134 mL 0.5671 mL 1.1341 mL 2.8354 mL
    25 mM 0.0907 mL 0.4537 mL 0.9073 mL 2.2683 mL
    30 mM 0.0756 mL 0.3780 mL 0.7561 mL 1.8902 mL
    40 mM 0.0567 mL 0.2835 mL 0.5671 mL 1.4177 mL
    50 mM 0.0454 mL 0.2268 mL 0.4537 mL 1.1341 mL
    60 mM 0.0378 mL 0.1890 mL 0.3780 mL 0.9451 mL
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    Ravoxertinib 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:

    Ravoxertinib1453848-26-4GDC-0994GDC0994GDC 0994ERKExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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