AVN-944

• CAT Number: I003029
• CAS Number: 297730-17-7
• Molecular Formula: C25H27N5O5
• Molecular Weight: 477.5
• Purity: ≥95%
• Synonyms: N-[(1S)-1-[3-[[[[3-methoxy-4-(5-oxazolyl)phenyl]amino]carbonyl]amino]phenyl]ethyl]-carbamic acid, (1R)-1-(cyanomethyl)propyl ester
• Target: IMPDH
• Solubility: DMSO: ≥ 58 mg/mL
• Storage: -20°C
• IC50: 6-10 nM (Ki) [1]
• InChI: InChI=1S/C25H27N5O5/c1-4-20(10-11-26)35-25(32)28-16(2)17-6-5-7-18(12-17)29-24(31)30-19-8-9-21(22(13-19)33-3)23-14-27-15-34-23/h5-9,12-16,20H,4,10H2,1-3H3,(H,28,32)(H2,29,30,31)/t16-,20+/m0/s1
• InChIKey: GYCPCOJTCINIFZ-OXJNMPFZSA-N
• SMILES: COC1=C(C2=CN=CO2)C=CC(NC(NC3=CC([C@@H](NC(O[C@H](CC)CC#N)=O)C)=CC=C3)=O)=C1

AVN-944(CAT: I003029) is a small molecule inhibitor of inosine monophosphate dehydrogenase (IMPDH), an enzyme involved in the de novo synthesis of guanosine nucleotides. By inhibiting IMPDH, AVN-944 disrupts the production of guanosine nucleotides, which are essential for DNA and RNA synthesis. This inhibition can lead to a depletion of intracellular guanosine triphosphate (GTP) levels and disrupt cellular processes that rely on GTP, particularly in rapidly dividing cells such as cancer cells. AVN-944 has demonstrated potential as an anticancer agent and has been studied in preclinical and clinical settings for the treatment of various malignancies. Further research is ongoing to evaluate its therapeutic efficacy and safety.

Reference

[1]. Zimmermann AG, et al. Inosine-5/’-monophosphate dehydrogenase: regulation of expression and role in cellular proliferation and T lymphocyte activation. Prog Nucleic Acid Res Mol Biol. 1998;61:181-209.
[2]. Huang M, et al. Guanine nucleotide depletion inhibits pre-ribosomal RNA synthesis and causes nucleolar disruption. Leuk Res. 2008 Jan;32(1):131-41.
[3]. Floryk D, et al. Antiproliferative effects of AVN944, a novel inosine 5-monophosphate dehydrogenase inhibitor, in prostate cancer cells. Int J Cancer. 2008 Nov 15;123(10):2294-302.