2. Apoptosis Cell Cycle/DNA Damage
  3. Thymidylate Synthase Antifolate
  4. ICI 198583

ICI 198583 is a thymidylate synthase (TS) inhibitor with a Ki value of 10 nM for both mouse and human TS. ICI 198583 serves as a substrate for folylpolyglutamate synthetase (FPGS) with a Km of 40 μM. ICI 198583 exerts persistent, dose-dependent inhibition on thymidylate synthase flux in mice. ICI 198583 is applicable to relevant research on leukemia.

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ICI 198583

ICI 198583 Chemical Structure

CAS No. : 112887-62-4

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ICI 198583 Related Antibodies

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Description

ICI 198583 is a thymidylate synthase (TS) inhibitor with a Ki value of 10 nM for both mouse and human TS. ICI 198583 serves as a substrate for folylpolyglutamate synthetase (FPGS) with a Km of 40 μM. ICI 198583 exerts persistent, dose-dependent inhibition on thymidylate synthase flux in mice. ICI 198583 is applicable to relevant research on leukemia[1].

Cellular Effect
Cell Line Type Value Description References
L1210 IC50
0.04 μM
Compound: 25a
Inhibition of thymidylate synthase from L1210 cells
Inhibition of thymidylate synthase from L1210 cells
[PMID: 1613755]
L1210 IC50
0.085 μM
Compound: 5
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
0.09 μM
Compound: 16
Inhibition concentration against L1210 cells
Inhibition concentration against L1210 cells
[PMID: 8230138]
L1210 IC50
0.09 μM
Compound: 1a
Growth inhibition of L1210 cells in culture.
Growth inhibition of L1210 cells in culture.
[PMID: 2231608]
L1210 IC50
0.09 μM
Compound: 2
Tested for the concentration to inhibit 50% of L1210 cell growth in culture.
Tested for the concentration to inhibit 50% of L1210 cell growth in culture.
[PMID: 2066994]
L1210 IC50
0.09 μM
Compound: 25a
The compound was tested in vitro for the inhibition of L1210 cell growth in culture
The compound was tested in vitro for the inhibition of L1210 cell growth in culture
[PMID: 1613755]
L1210 IC50
0.09 μM
Compound: 2a
In vitro inhibition of L1210 cell growth in culture.
In vitro inhibition of L1210 cell growth in culture.
[PMID: 2033585]
L1210 IC50
0.09 μM
Compound: 3a
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
0.13 μM
Compound: 3
Growth inhibition of murine tumor L1210 cell line
Growth inhibition of murine tumor L1210 cell line
[PMID: 10508430]
L1210 IC50
40 nM
Compound: 3
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 (1565) IC50
8.2 μM
Compound: 3
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 (1565) IC50
8.3 μM
Compound: 5
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 (R7A) IC50
0.39 μM
Compound: 5
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
2.7 μM
Compound: 3
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]
In Vitro

ICI 198583 potently inhibits partially purified murine thymidylate synthase (TS) and human thymidylate synthase (TS), with a Ki of 10 nM[1].
ICI 198583 serves as a substrate for partially purified mouse liver FPGS, with a Km of 40 μM[1].
ICI 198583 potently inhibits the proliferation of L1210 cells (IC50 = 0.085 μM) and W1L2 cells (IC50 = 0.056 μM) in vitro. It remains active against L1210:R7A cells overexpressing DHFR, while its activity against reduced folate transport-deficient L1210:1565 cells decreases by 96-fold[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ICI 198583 Related Antibodies
Parmacokinetics
Species Dose Route T1/2β AUC0-∞ CL
Mice[1] 500 mg/kg i.v. 16 min 393 μM·h 42 mL/min/kg
In Vivo

ICI 198583 (1-50 mg/kg; i.p.; once daily; for 5 consecutive days) exhibits potent therapeutic activity against L1210:ICR leukemia in male C57BL×DBA2 F1 hybrid mice[1].
ICI 198583 (50-500 mg/kg; intravenous injection; single bolus) produces dose-dependent, sustained inhibition of thymidylate synthase in L1210:NCI leukemia cells of male C57BL×DBA2 F1 hybrid mice. After a single intravenous bolus of 500 mg/kg, the inhibition rate remains above 80% for 24 hours[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL×DBA2 F1 hybrid (male; leukemia model via i.p. injection of 5×104 L1210:ICR tumor cells)[1]
Dosage: 5 mg/kg; 10 mg/kg; 50 mg/kg; >500 mg/kg
Administration: i.p.; daily; 5 days
Result: Cured 4/7 mice at 5 mg/kg daily for 5 days.
Cured 4/7 mice at 10 mg/kg daily for 5 days.
Cured 6/7 mice at 50 mg/kg daily for 5 days.
Exhibited a maximum tolerated dose >500 mg/kg daily for 5 days, with only 10% body weight loss observed at this dose.
Molecular Weight

476.48

Formula

C25H24N4O6
CAS No.
SMILES

O=C(CC[C@H](NC(C1=CC=C(C=C1)N(CC#C)CC2=CC3=C(C=C2)NC(C)=NC3=O)=O)C(O)=O)O
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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ICI 198583 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:

ICI 198583112887-62-4ICI198583ICI-198583Thymidylate SynthaseAntifolatereduced folate/methotrexate transport systemmurine L1210 cellsfolylpolyglutamate synthetasemouse thymidylate synthaseL1210:C15 thymidylate synthaseW1L2:C1 thymidylate synthasehuman W1L2 cellsleukemiathymidylate synthasehuman thymidylate synthaseInhibitorinhibitorinhibit

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