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

GDC-0994 (Synonyms: Ravoxertinib)

Cat. No.: HY-15947 Purity: 99.57%
Data Sheet SDS 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 $88 In-stock
5 mg $80 In-stock
10 mg $100 In-stock
50 mg $300 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Other Forms of GDC-0994:

  • 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

IC50: 6.1 nM (ERK1), 3.1 nM (ERK2), 12 nM (p90RSK)[1]

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
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References
Preparing Stock Solutions
Concentration Volume 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.
Animal Administration
[1]

GDC-0994 is prepared in 40% PEG400/60% (10% HPβCD) (Mice)[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

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

Solvent & Solubility

DMSO: ≥ 35 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.57%

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