Basic information Safety Supplier Related

Lometrexol

Basic information Safety Supplier Related

Lometrexol Basic information

Product Name:
Lometrexol
Synonyms:
  • Lometrexol
  • (6R)-5,10-Dideaza-5,6,7,8-tetrahydrofolic acid
  • N-[4-[2-[[(6R)-2-Amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin]-6-yl]ethyl]benzoyl]-L-glutamic acid
  • N-[4-[2-[[(R)-2-Amino-4-oxo-1,4,5,6,7,8-hexahydropyrido[2,3-d]pyrimidin]-6-yl]ethyl]benzoyl]-L-glutamic acid
  • L-Glutamic acid, N-(4-(2-((6R)-2-amino-1,4,5,6,7,8-hexahydro-4-oxopyrido(2,3-D)pyrimidin-6-yl)ethyl)benzoyl)-
  • L-Glutamic acid, N-(4-(2-(2-amino-1,4,5,6,7,8-hexahydro-4-oxopyrido(2,3-D)pyrimidin-6-yl)ethyl)benzoyl)-, (R)-
  • Lometrexolum
  • Lometrexolum [inn-latin]
CAS:
106400-81-1
MF:
C21H25N5O6
MW:
443.45
Product Categories:
  • Aromatics
  • Chiral Reagents
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
Mol File:
106400-81-1.mol
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Lometrexol Chemical Properties

Density 
1.56±0.1 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
DMSO: ≥5mg/mL
pka
3.60±0.10(Predicted)
form 
powder
color 
white to light yellow
Stability:
Hygroscopic
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Safety Information

Hazard Codes 
T
Risk Statements 
25
Safety Statements 
45
RIDADR 
UN 2811 6.1 / PGIII
WGK Germany 
3
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Lometrexol Usage And Synthesis

Description

Glycinamide ribonucleotide formyltransferase (GART) is a folate-dependent enzyme required for de novo purine synthesis. Lometrexol is a folate analog antimetabolite with antineoplastic activity. At nanomolar conentrations, it inhibits GART preventing de novo purine synthesis, inhibiting DNA synthesis, arresting cells in the S phase of the cell cycle, and inhibiting tumor cell proliferation.

Uses

Lometrexol hydrate was used to compare the biological activity of potent inhibitor of human GARFTase.

Uses

It is an antifolate which inhibits glycinamide ribonucleotide formyltransferase (GARFT), an enzyme essential for de novo purine synthesis.

Biochem/physiol Actions

Glycinamide Ribonucleotide Formyltransferase (GARFTase) is a folate-dependent enzyme required for de novo purine synthesis. Lometrexate is a potent inhibitor of GARFTase, but does not interfere with enzymes involved in the synthesis of folate. Lometrexerol has been tested clinically for the treatment of various cancers as an anti-folate like agent, similar to methotrexate. Treatment with lometrexol rapidly decreases ATP and GTP levels, cell cycle arrest and induces apoptosis. Although depletion of nucleotide pools induces p53 expression, lometrexol is cytotoxic in both wild-type and mutant p53 expressing tumor cells. Lometrexol is cytotoxic in CCRF-CEm leukemia cells with an IC50 of 2.9 nM.

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