2. Apoptosis
  3. Thymidylate Synthase
  4. 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.

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CB 3717

CB 3717 Chemical Structure

CAS No. : 76849-19-9

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CB 3717 Related Antibodies

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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].

Cellular Effect
Cell Line Type Value Description References
K562 IC50
0.037 μM
Compound: 1 (5,8-deaza-10-propargylfolate)
Ability to inhibit thymidylate synthase derived from human leukemia K562 cells
Ability to inhibit thymidylate synthase derived from human leukemia K562 cells
[PMID: 3470522]
L1210 IC50
0.02 μM
Compound: 1 (CB-3717)
In vitro inhibitory activity against thymidylate synthase (TS) from L1210 mouse leukemia cells
In vitro inhibitory activity against thymidylate synthase (TS) from L1210 mouse leukemia cells
[PMID: 1495009]
L1210 IC50
20 nM
Compound: 2
Inhibition of isolated thymidylate synthase partially purified from L1210 mouse leukemia cells
Inhibition of isolated thymidylate synthase partially purified from L1210 mouse leukemia cells
[PMID: 10508430]
L1210 IC50
3.4 μM
Compound: 1 (CB-3717)
In vitro inhibition of L1210 mouse leukemia cell growth in culture
In vitro inhibition of L1210 mouse leukemia cell growth in culture
[PMID: 1495009]
L1210 IC50
3.4 μM
Compound: 15
Inhibition concentration against L1210 cells
Inhibition concentration against L1210 cells
[PMID: 8230138]
L1210 IC50
3.4 μM
Compound: 1a
Concentration required to inhibit 50 percent growth of L1210 mouse leukemia cells
Concentration required to inhibit 50 percent growth of L1210 mouse leukemia cells
[PMID: 2231606]
L1210 IC50
3.5 μM
Compound: 1
Concentration required to inhibit 50% growth of L1210 mouse leukemia cells was determined
Concentration required to inhibit 50% growth of L1210 mouse leukemia cells was determined
[PMID: 2231607]
L1210 IC50
5.5 μM
Compound: 2
Growth inhibition of murine tumor L1210 cell line
Growth inhibition of murine tumor L1210 cell line
[PMID: 10508430]
L1210 (1565) IC50
3.6 μM
Compound: 1
Concentration required to inhibit 50% growth of L1210 /1565 mutant mouse leukemia cell line was determined
Concentration required to inhibit 50% growth of L1210 /1565 mutant mouse leukemia cell line was determined
[PMID: 2231607]
L1210 (1565) IC50
5.5 μM
Compound: 2
Inhibition of cell growth in culture against murine tumor L1210:1565 cell lines
Inhibition of cell growth in culture against murine tumor L1210:1565 cell lines
[PMID: 10508430]
L1210 (R7A) IC50
41 μM
Compound: 1
Concentration required to inhibit 50% growth of L1210 of R7A mutant mouse leukemia cell line was determined
Concentration required to inhibit 50% growth of L1210 of R7A mutant mouse leukemia cell line was determined
[PMID: 2231607]
L1210 (RD1694) IC50
13 μM
Compound: 2
Tested for inhibition of cell growth in culture against murine tumor L1210:RD1694 cell lines
Tested for inhibition of cell growth in culture against murine tumor L1210:RD1694 cell lines
[PMID: 10508430]
WIL2 IC50
0.44 μM
Compound: 1 (CB-3717)
Inhibition of human derived cell line W1-L2 cell proliferation
Inhibition of human derived cell line W1-L2 cell proliferation
[PMID: 1495009]
Molecular Weight

477.47

Formula

C24H23N5O6
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CB 3717 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CB 371776849-19-9PDDFCB3717CB-3717Thymidylate SynthaseInhibitorinhibitorinhibit

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