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

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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

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Safety

HS Code: 2924297099

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-5092
Product name: Ravoxertinibhydrochloride
Purity: 98.99%
Packaging: 5mg
Price: $96
Updated: 2021/12/16

ChemScene

Product number: CS-5092
Product name: Ravoxertinibhydrochloride
Purity: 98.99%
Packaging: 10mg
Price: $120
Updated: 2021/12/16

ChemScene

Product number: CS-5092
Product name: Ravoxertinibhydrochloride
Purity: 98.99%
Packaging: 50mg
Price: $360
Updated: 2021/12/16

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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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GDC-0994 (hydrochloride) Suppliers

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2070009-58-2, GDC-0994 (hydrochloride)Related Search:

GDC-0994 (hydrochloride)

GDC-0994 HCl

CS-2072

Ravoxertinib hydrochloride

RAVOXERTINIB HYDROCHLORIDE (GDC-0994 HYDROCHLORIDE)

Ravoxertinib hydrochloride (GDC-0994

2070009-58-2