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Lometrexol

Cat. No. M27736

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Lometrexol Structure
Synonym:

DDATHF

Size Price Availability Quantity
1mg USD 100  USD100 In stock
5mg USD 250  USD250 In stock
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Quality Control & Documentation
Biological Activity

Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.

Chemical Information
Molecular Weight 443.45
Formula C21H25N5O6
CAS Number 106400-81-1
Form Solid
Solubility (25°C) DMSO ≥ 40 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] J D Roberts, et al. Cancer Chemother Pharmacol. Weekly lometrexol with daily oral folic acid is appropriate for phase II evaluation

[2] C Sessa, et al. Clin Cancer Res. Phase I study of the antipurine antifolate lometrexol (DDATHF) with folinic acid rescue

[3] T W Synold, et al. Clin Cancer Res. Cellular but not plasma pharmacokinetics of lometrexol correlate with the occurrence of cumulative hematological toxicity

[4] L G Mendelsohn, et al. Invest New Drugs. Biochemistry and pharmacology of glycinamide ribonucleotide formyltransferase inhibitors: LY309887 and lometrexol

[5] T Alati, et al. Cancer Res. Augmentation of the therapeutic activity of lometrexol -(6-R)5,10-dideazatetrahydrofolate- by oral folic acid

Related Antifolate Products
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Methotrexate α-tert-butyl ester 

Methotrexate α-tert-butyl ester, capped by OtBu, significantly reduces tumor growth in HT1080 tumor bearing mice.

Trimetrexate glucuronate

Trimetrexate glucuronate (NSC 352122) is a folic acid antagonist. Trimetrexate glucuronate affects DNA and RNA synthesis by inhibiting dihydrofolate reductase and preventing the synthesis of purine nucleotides and thymidylate. Trimetrexate glucuronate has potential antitumour activity and can also be used to inhibit Pneumocystis carinii pneumonia.

Pemetrexed disodium heptahydrate

Pemetrexed disodium heptahydrate is a novel antifolate, the Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.

Fanotaprim

Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor with IC50s of 1.57 and 308 nM for tgDHFR (Toxoplasma gondii DHFR) and hDHFR (human DHFR), respectively. Fanotaprim has the potential for the research of toxoplasmosis.

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Keywords: Lometrexol, DDATHF supplier, Antifolate, inhibitors, activators

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