145788-82-5

CB30900 is a novel, potent thymidylate synthase inhibitor. CB30900 is a TS inhibitor that does not rely on polyglutamation for activity. Greater than 90% TS inhibition was achieved following a 4-hr exposure to each compound at equitoxic doses (up to 100 times the IC50 determine by a 48-hr growth inhibition assay).

CB30900 is an inhibitor for thymidylate synthase with an IC50 of 0.2 μM. CB30900 exhibits cytotoxicity in W1L2 with an IC50 of 0.13 μM[1][2].

[1] Walton MI, et al., Preclinical pharmacology of CB30900, a novel dipeptide inhibitor of thymidylate synthase, in mice. J Pharmacol Exp Ther. 1996 May;277(2):909-16. PMID:8627573
[2] Aherne GW, et al., Immunoreactive dUMP and TTP pools as an index of thymidylate synthase inhibition; effect of tomudex (ZD1694) and a nonpolyglutamated quinazoline antifolate (CB30900) in L1210 mouse leukaemia cells. Biochem Pharmacol. 1996 May 17;51(10):1293-301 DOI:10.1016/0006-2952(96)00035-4