Nolatrexed (hydrochloride)

Nolatrexed is a thymidylate synthase inhibitor (Ki = 11 nM). It inhibits cell growth in a panel of human and murine cancer cell lines (IC50s = 0.39-6.6 µM). Nolatrexed inhibits the growth of L1210 cells, an effect that is decreased by greater than 50-fold by the addition of exogenous thymidine. Nolatrexed (0.7 and 3.5 µM) induces cell cycle arrest at the S phase in L1210 cells. It increases life span in a thymidine kinase-deficient L5178Y/TK- murine lymphoma model when administered at doses ranging from 25 to 200 mg/kg.Formal Name: 2-amino-6-methyl-5-(4-pyridinylthio)-4(1H)-quinazolinone, dihydrochloride. CAS Number: 152946-68-4. Synonyms: AG337. Molecular Formula: C14H12N4OS . 2HCl. Formula Weight: 357.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 15 mg/ml, DMSO:PBS (pH 7.2) (1:8): 0.11 mg/ml. lambdamax: 232, 273 nm. SMILES: NC1=NC(C2=C(SC3=CC=NC=C3)C(C)=CC=C2N1)=O.Cl.Cl. InChi Code: 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. InChi Key: PJKVJJYMWOCLIJ-UHFFFAOYSA-N.