| Company Name: |
Musechem |
| Tel: |
+1-800-259-7612 |
| Email: |
info@musechem.com |
|
| | GDC-0994 (hydrochloride) Basic information |
| Product Name: | GDC-0994 (hydrochloride) | | Synonyms: | GDC-0994 (hydrochloride);GDC-0994 HCl;CS-2072;Ravoxertinib hydrochloride;RAVOXERTINIB HYDROCHLORIDE (GDC-0994 HYDROCHLORIDE);Ravoxertinib hydrochloride (GDC-0994 | | CAS: | 2070009-58-2 | | MF: | C21H19Cl2FN6O2 | | MW: | 477.32 | | EINECS: | | | Product Categories: | | | Mol File: | 2070009-58-2.mol |  |
| | GDC-0994 (hydrochloride) Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO: 100 mg/mL (209.50 mM) | | form | Solid | | color | Light yellow to yellow |
| | GDC-0994 (hydrochloride) Usage And Synthesis |
| 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 |
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