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Cat. No.: HY-113798

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ICI 198583

ICI 198583 is a thymidylate synthase (TS) inhibitor with a K_i value of 10 nM for both mouse and human TS. ICI 198583 serves as a substrate for folylpolyglutamate synthetase (FPGS) with a K_m 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.

For research use only. We do not sell to patients.

CAS No.: 112887-62-4
Formula: C₂₅H₂₄N₄O₆
Molecular Weight:476.48

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Please store the product under the recommended conditions in the Certificate of Analysis.

ICI 198583 Chemical Structure

CAS No.: 112887-62-4

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Biological Activity
- Description
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
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Biological Activity

Description

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 K_i of 10 nM^[1].
ICI 198583 serves as a substrate for partially purified mouse liver FPGS, with a K_m 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.

Parmacokinetics

Species	Dose	Route	T_1/2β	AUC_0-∞	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.

Chemical Information

CAS No. 112887-62-4
Molecular Weight 476.48
Formula C₂₅H₂₄N₄O₆
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
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Jackman AL, et al. The biochemical pharmacology of the thymidylate synthase inhibitor, 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583). Biochem Pharmacol. 1991 Oct 24;42(10):1885-95. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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