Nolatrexed Dihydrochloride

• CAT Number: R008557
• CAS Number: 152946-68-4
• Molecular Formula: C14H14Cl2N4OS
• Molecular Weight: 357.253
• Purity: ≥95%
• Synonyms: 2-Amino-6-methyl-5-(4-pyridinylthio)-4(1H)-quinazolinone Hydrochloride; AG 337; Thymitaq
• Target: Thymidylate Synthase
• Solubility: >17.2mg/mL in DMSO
• Storage: Store at -20°C
• IUPAC Name: 2-amino-6-methyl-5-pyridin-4-ylsulfanyl-1H-quinazolin-4-one;dihydrochloride
• InChI: InChI=1S/C14H12N4OS.2ClH/c1-8-2-3-10-11(13(19)18-14(15)17-10)12(8)20-9-4-6-16-7-5-9;;/h2-7H,1H3,(H3,15,17,18,19);2*1H
• InChIKey: PJKVJJYMWOCLIJ-UHFFFAOYSA-N
• SMILES: CC1=C(C2=C(C=C1)NC(=NC2=O)N)SC3=CC=NC=C3.Cl.Cl

Nolatrexed Dihydrochloride (CAS 152946-68-4) is the dihydrochloride salt of nolatrexed, a water-soluble lipophilic quinazoline folate analog with antineoplastic activity. Nolatrexed occupies the folate binding site of thymidylate synthase, resulting in inhibition of thymidylate synthase activity and thymine nucleotide synthesis with subsequent inhibition of DNA replication, DNA damage, S-phase cell cycle arrest, and caspase-dependent apoptosis. Its synergistic anticancer effect has reported.

Overview of Clinical Research

Nolatrexed Dihydrochloride is a Thymidylate synthase inhibitor developed by Agouron Pharmaceuticals. Nolatrexed or 5-fluorouracil in combination with cisplatin in patients with nasopharyngeal cancer was completed in 2015.

Reference

1. Rafi, Imran, et al. "Preclinical and phase I clinical studies with the nonclassical antifolate thymidylate synthase inhibitor nolatrexed dihydrochloride given by prolonged administration in patients with solid tumors." Journal of clinical oncology 16.3 (1998): 1131-1141.
2.Hy, Tu, and Chen Wm. "Synergistic anticancer effect of sodium phenylbutyrate combined with nolatrexed dihydrochloride in vitro." Life Science Research 7.4 (2003): 346-349.
3.Chen, S. Z., S. M. Wang, and J. R. Zhang. "Preparation of long-circulating nolatrexed dihydrochloride liposomes and its antitumor activity." Journal of Southern Medical University 28.3 (2008): 403-405.
4.LU, Hui-min, Wei-xia DU, and Ying-hua FU. "Inhibition Effect of Nolatrexed Dihydrochloride on Transplatation Tumors." Journal of Preventive Medicine Information 4 (2007): 8.