501345-02-4

Basic information

• Product Name: AVN-944
• Synonyms: AVN-944
• CAS NO: 501345-02-4
• Molecular Formula: C25H27N5O5
• Molecular Weight: 477.51238
• Mol File: 501345-02-4.mol
• Article Data: 0

Chemical Properties

• Boiling Point: 587.76 °C at 760 mmHg
• Flash Point: 309.266 °C
• Appearance: /
• Density: 1.297 g/cm³
• CAS DataBase Reference: AVN-944(CAS DataBase Reference)
• NIST Chemistry Reference: AVN-944(501345-02-4)
• EPA Substance Registry System: AVN-944(501345-02-4)

Safety Data

• Hazardous Substances Data: 501345-02-4(Hazardous Substances Data)

Usage

Description

AVN-944 is a novel inosine monophosphate dehydrogenase (IMPDH) inhibitor, characterized by its antiproliferative effects and potential for combination with other agents in the treatment of human prostate cancer. It is also suitable for pyruvate dehydrogenase (PDH) related research.

Uses

Used in Pharmaceutical Industry:
AVN-944 is used as an IMPDH inhibitor for its antiproliferative effects, making it a promising candidate in the treatment of human prostate cancer. It can be combined with other agents to enhance the therapeutic outcomes for patients.
Used in Research Applications:
AVN-944 is used as a research tool for studying pyruvate dehydrogenase (PDH) related processes. Its role as an IMPDH inhibitor allows researchers to investigate the effects of this enzyme on various cellular functions and pathways, contributing to a better understanding of its role in disease mechanisms and potential therapeutic targets.

Enzyme inhibitor

This orally available antineoplastic agent (FW = 310.36 g/mol; CAS 297730-17-7), also known as VX-944 and (R) -1-cyanobutan-2-yl- (S) -1- (3- (3- (3-methoxy-4- (oxazol-5-yl) phenyl) ureido) phenyl) ethyl) carbamate, inhibits inosine 5’-monophosphate dehydrogenase (IMPDH), the enzyme catalyzing the conversion of IMP into XMP, leading to the biosynthesis of GMP, GDP, GTP, and ultimately dGTP. IMPDH is overexpressed in some cancer cells, particularly in hematological malignancies, and AVN944 appears to have a selective cytotoxic effect on cancer cells. Reduction of GTP in normal cells results in a temporary slowing of cell growth only. AVN944 treatment results in dose-dependent cell growth inhibition in all studied prostate cancer cells, independently of their androgen sensitivity . AVN944 treatment arrests LNCaP cells in G1-phase and and androgen- independent 22Rv1, DU145 and PC-3 cells in S-phase. AVN-944 treatment leads to the rapid disappearance of nucleostemin, a positive regulator of cell proliferation that is highly expressed in a variety of stem cells, tumors, and tumor cell lines.