CB 3717

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 Specifications

CAS Number

[76849-19-9]

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