1453848-26-4

Basic information

• Product Name: GDC-0994
• Synonyms: GDC-0994;(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;(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;1-[(1S)-1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[2-[(1-methyl-1H-pyrazol-5-yl)amino]-4-pyrimidinyl]-2(1H)-pyridinone;Ravoxertinib;EOS-60648
• CAS NO: 1453848-26-4
• Molecular Formula: C₂₁H₁₈ClFN₆O₂
• Molecular Weight: 440.8580232
• Product Categories: Inhibitors
• Mol File: 1453848-26-4.mol
• Article Data: 4

Chemical Properties

• Boiling Point: 734.6±70.0 °C(Predicted)
• Appearance: /
• Density: 1.45±0.1 g/cm3(Predicted)
• Solubility: ≥44.1 mg/mL in DMSO; insoluble in H2O; ≥19.2 mg/mL in EtOH
• PKA: 14.03±0.10(Predicted)
• CAS DataBase Reference: GDC-0994(CAS DataBase Reference)
• NIST Chemistry Reference: GDC-0994(1453848-26-4)
• EPA Substance Registry System: GDC-0994(1453848-26-4)

Safety Data

• Hazardous Substances Data: 1453848-26-4(Hazardous Substances Data)

Usage

Description

GDC-0994 is a potent and selective ERK1 and ERK2 inhibitor with IC50 values of 6.1 and 4.1 nM, respectively. It is an orally available compound that has demonstrated the ability to inhibit ERK-dependent tumor cell proliferation and survival, making it a promising candidate for cancer treatment.

Uses

Used in Anticancer Applications:
GDC-0994 is used as an anticancer agent for its ability to prevent ERK-dependent tumor cell proliferation and survival. It has shown significant inhibition of tumor growth in HCT116 human colorectal cancer xenograft tumors, with an 80% reduction in growth observed at a dosage of 100 mg/kg when administered orally once daily for 21 days.
Used in Pharmaceutical Research:
GDC-0994 is used as a research tool in the pharmaceutical industry for studying the role of ERK1 and ERK2 in various cellular processes and their potential as therapeutic targets for cancer treatment. Its potent and selective inhibition of these proteins allows researchers to better understand the underlying mechanisms of cancer development and progression, leading to the development of more effective treatment strategies.

references

[1]. robarge k, schwarz j, blake j, et al. abstract ddt02-03: discovery of gdc-0994, a potent and selective erk1/2 inhibitor in early clinical development. aacr annual meeting, 2014, san diego, ca.

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Relevant articles and documents

PROCESS FOR THE MANUFACTURING OF MEDICAMENTS

The present invention provides a process for the manufacture of a compound of formula VIIIa and salts forms of VIIIa where Rc is an aryl sulfonic acid

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 Development

The extracellular signal-regulated kinases ERK1/2 represent an essential node within the RAS/RAF/MEK/ERK signaling cascade that is commonly activated by oncogenic mutations in BRAF or RAS or by upstream oncogenic signaling. While targeting upstream nodes