| Identification | Back Directory | [Name]
GDC-0994 (hydrochloride) | [CAS]
2070009-58-2 | [Synonyms]
CS-2072
GDC-0994 HCl
GDC-0994 (hydrochloride)
Ravoxertinib hydrochloride
RAVOXERTINIB HYDROCHLORIDE (GDC-0994 HYDROCHLORIDE) | [Molecular Formula]
C21H19Cl2FN6O2 | [MDL Number]
MFCD29472257 | [MOL File]
2070009-58-2.mol | [Molecular Weight]
477.32 |
| Hazard Information | Back Directory | [Uses]
Ravoxertinib hydrochloride (GDC-0994 hydrochloride) 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. | [in vivo]
In CD-1 mice, a 10 mg/kg oral dose of Ravoxertinib 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]. | [IC 50]
ERK2: 3.1 nM (IC50); ERK1: 6.1 nM (IC50); p-RSK: 12 nM (IC50) | [References]
[1] Blake JF, et al. Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Developme DOI:10.1021/acs.jmedchem.6b00389
[2] Kirk Robarge, et al. Abstract DDT02-03: Discovery of GDC-0994, a potent and selective ERK1/2 inhibitor in early clinical development. Proceedings: AACR Annual Meeting 2014; April 5-9, 2014.
[3] MICHAEL LAI. Opportunity for Pharmaceutical Intervention in Lung Cancer: Selective Inhibition of JAK1/2 to Eliminate EMT-Derived Mesenchymal Cells. |
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| Company Name: |
Musechem
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| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
| Company Name: |
Cckinase, Inc.
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+1 (732)236-3202 |
| Website: |
www.cckinase.com |
| Company Name: |
cjbscvictory
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13348960310 |
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https://www.weikeqi-biotech.com/ |
| Company Name: |
InvivoChem
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| Tel: |
13549236410 |
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https://www.invivochem.cn/ |
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