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Ravoxertinib hydrochloride(GDC-0994 RG7842)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ravoxertinib hydrochloride(GDC-0994 RG7842)图片
CAS NO:2070009-58-2
规格:≥98%
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)477.32
FormulaC21H19Cl2FN6O2
CAS No.2070009-58-2
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO:> 100 mg/mL
Water: N/A
Ethanol: N/A
Solubility (In vivo) 2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 30 mg/mL
Synonyms RG 7842 HCl; GDC0994; GDC-0994; GDC 0994; RG7842; RG-7842; RG 7842
实验参考方法
In Vitro

In vitro activity: GDC-0994, also known as ravoxertinib and RG7842, is a potent, orally available ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. It has demonstrated anticancer activity. Upon oral administration, GDC-0994 inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways. This prevents ERK-dependent tumor cell proliferation and survival.


Kinase Assay: 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. 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.


Cell Assay: GDC-0994 potently inhibits phospho-p90RSK in tumor cells.

In VivoGDC-0994 (p.o.) results in significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice. In vivo, GDC-0994 (p.o.) inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways, and subsequently prevents ERK-dependent tumor cell proliferation and survival.
Animal modelPK/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.
Formulation & DosageDissolved in 40% PEG400/60% (10% HPβCD); 15, 30, or 100 mg/kg; oral
ReferencesJ Med Chem. 2016 Jun 23;59(12):5650-60.