CB 3717

• Description :

  CB 3717 is a potent inhibitor of human thymidylate synthetase, competitively binding with 5,10-methylenetetrahydrofolate (Ki = 4.9 X 10 (-9) M) . It also competitively inhibits human dihydrofolate reductase with dihydrofolate (Ki = 2.3 X 10 (-8) M) . In WI-L2 human lymphoblastoid cells, CB 3717 treatment led to a significant decrease in cellular dTTP levels and a notable increase in dUMP levels, indicating a disruption in nucleotide metabolism. The growth-inhibitory effect of CB 3717 was reversed by thymidine supplementation, demonstrating that thymidylate synthetase became rate-limiting in the presence of this compound. Delayed thymidine supplementation beyond 8 hours resulted in severe cytotoxicity, underscoring the critical timing of nucleotide rescue strategies in CB 3717-treated cells[1].

• Product Name Alternative :

  PDDF

• UNSPSC :

  12352005

• Target :

  Thymidylate Synthase

• Type :

  Reference compound

• Related Pathways :

  Apoptosis

• Applications :

  Metabolism-protein/nucleotide metabolism

• Field of Research :

  Metabolic Disease

• Assay Protocol :

  https://www.medchemexpress.com/cb-3717.html

• Smiles :

  O=C1C2=CC(CN(C3=CC=C(C=C3)C(N[C@H](C(O)=O)CCC(O)=O)=O)CC#C)=CC=C2NC(N)=N1

• Molecular Formula :

  C24H23N5O6

• Molecular Weight :

  477.47

• References & Citations :

  [1]Biochemical effects of a quinazoline inhibitor of thymidylate synthetase, N- (4- (N- ((2-amino-4-hydroxy-6-quinazolinyl) methyl) prop-2-ynylamino) benzoyl) -L-glutamic acid (CB3717), on human lymphoblastoid cells

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• CAS Number :

  [76849-19-9]