GDC-0994 (hydrochloride)
- Product Name
- GDC-0994 (hydrochloride)
- CAS No.
- 2070009-58-2
- Chemical Name
- GDC-0994 (hydrochloride)
- Synonyms
- CS-2072;GDC-0994 HCl;GDC-0994 (hydrochloride);Ravoxertinib hydrochloride;Ravoxertinib hydrochloride (GDC-0994;RAVOXERTINIB HYDROCHLORIDE (GDC-0994 HYDROCHLORIDE)
- CBNumber
- CB73048653
- Molecular Formula
- C21H19Cl2FN6O2
- Formula Weight
- 477.32
- MOL File
- 2070009-58-2.mol
GDC-0994 (hydrochloride) Property
- storage temp.
- Store at -20°C
- solubility
- DMSO: 100 mg/mL (209.50 mM)
- form
- Solid
- color
- Light yellow to yellow
Safety
- HS Code
- 2924297099
N-Bromosuccinimide Price
- Product number
- CS-5092
- Product name
- Ravoxertinibhydrochloride
- Purity
- 98.99%
- Packaging
- 5mg
- Price
- $96
- Updated
- 2021/12/16
- Product number
- CS-5092
- Product name
- Ravoxertinibhydrochloride
- Purity
- 98.99%
- Packaging
- 10mg
- Price
- $120
- Updated
- 2021/12/16
- Product number
- CS-5092
- Product name
- Ravoxertinibhydrochloride
- Purity
- 98.99%
- Packaging
- 50mg
- Price
- $360
- Updated
- 2021/12/16
GDC-0994 (hydrochloride) Chemical Properties,Usage,Production
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.
GDC-0994 (hydrochloride) Preparation Products And Raw materials
Raw materials
Preparation Products
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