GDC-0994

SKU: orb1226241

Description

GDC-0994 is a potent, orally available ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.(In Vitro):Ravoxertinib (GDC-0994) also inhibits p90RSK with an IC50 of 12 nM.Ravoxertinib (GDC-0994) is highly selective for ERK1 and ERK2, with biochemical potency of 1.1 nM and 0.3 nM, respectively.Ravoxertinib (GDC0994; 50 nM, 0.5 μM, and 5 μM; 48 hours) decreases the viability of lung adenocarcinoma cell lines (A549, HCC827, HCC4006).(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. 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.

Key Properties

• CAS Number: 1453848-26-4
• MW: 440.864
• Purity: >98% (HPLC)
• Formula: C₂₁H₁₈ClFN₆O₂
• SMILES: O=C1C=C(C2=NC(NC3=CC=NN3C)=NC=C2)C=CN1[C@@H](C4=CC=C(Cl)C(F)=C4)CO
• Target: ERK
• Solubility: Ethanol: 87 mg/mL (197.79 mM); DMSO: 87 mg/mL (197.79 mM)

Bioactivity

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

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RG-7842

Quick Database Links

Gene Symbol

ERK