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BIOLOGICAL INFO
Solubility:
DMSO: =40 mg/mL
Application(s):
Thymidylate synthase inhibitor
REVIEW Raltitrexed is an antineoplastic Agents and folic acid antagonists. Raltitrexed inhibits thymidylate synthase (TS) leading to DNA fragmentation and cell death. It is transported into cells via a reduced folate carrier. Inside the cell Raltitrexed is extensively polyglutamated, which enhances thymidylate synthase inhibitory power and duration. Inhibition of this enzyme results in decreased synthesis of thymidine triphosphate which is required for DNA synthesis.
REFERENCES
[1]
Widemann BC, Balis FM, Godwin KS, McCully C, Adamson PC (1999). The plasma pharmacokinetics and cerebrospinal fluid penetration of the thymidylate synthase inhibitor raltitrexed (Tomudex) in a nonhuman primate model. Cancer Chemother. Pharmacol. 44 (6): 439-43. PMID 10550563.
[2]
Calvert AH, Alison DL, Harland SJ, et al. (August 1986). A phase I evaluation of the quinazoline antifolate thymidylate synthase inhibitor, N10-propargyl-5,8-dideazafolic acid, CB3717. J. Clin. Oncol. 4 (8): 1245-52. PMID 3734849.
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