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

Ravoxertinib (Synonyms: GDC-0994)

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

Ravoxertinib (GDC-0994) is an orally bioavailable 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.

Ravoxertinib Chemical Structure

Ravoxertinib Chemical Structure

CAS No. : 1453848-26-4

Size Price Stock Quantity
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  

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Customer Review

Based on 4 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

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  • References

Description

Ravoxertinib (GDC-0994) is an orally bioavailable 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)

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].

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].

Clinical Trial
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 : ≥ 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 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
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

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.79%

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Product Name:
Ravoxertinib
Cat. No.:
HY-15947
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Ravoxertinib

Cat. No.: HY-15947