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Lometrexol

Product Name
Lometrexol
CAS No.
106400-81-1
Chemical Name
Lometrexol
Synonyms
LY 264618;Lometrexol;Lometrexolum;LY 264618 hydrate;Lometrexol hydrate;Lometrexol(LY 264618);Lometrexolum [inn-latin];(6R)-5,10-Dideaza-5,6,7,8-tetrahydrofolic 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)-
CBNumber
CB81179064
Molecular Formula
C21H25N5O6
Formula Weight
443.45
MOL File
106400-81-1.mol
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Lometrexol Property

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

Hazard Codes 
T
Risk Statements 
25
Safety Statements 
45
RIDADR 
UN 2811 6.1 / PGIII
WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H301Toxic if swalloed

Precautionary statements

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0040
Product name
Lometrexol hydrate
Purity
≥95% (HPLC)
Packaging
5mg
Price
$254
Updated
2024/03/01
Sigma-Aldrich
Product number
SML0040
Product name
Lometrexol hydrate
Purity
≥95% (HPLC)
Packaging
25mg
Price
$666
Updated
2024/03/01
Cayman Chemical
Product number
18049
Product name
Lometrexol
Purity
≥98%
Packaging
1mg
Price
$97
Updated
2024/03/01
Cayman Chemical
Product number
18049
Product name
Lometrexol
Purity
≥98%
Packaging
5mg
Price
$243
Updated
2024/03/01
ChemScene
Product number
CS-0003423
Product name
Lometrexol
Packaging
1mg
Price
$275
Updated
2021/12/16
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Lometrexol Chemical Properties,Usage,Production

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.

Lometrexol Preparation Products And Raw materials

Raw materials

Preparation Products

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Lometrexol Suppliers

J & K SCIENTIFIC LTD.
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+86-400-002-6226 +86-13028896684;
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021-58447131 13564518121
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RD International Technology Co., Limited
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106400-81-1, LometrexolRelated Search:


  • 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]
  • LY 264618
  • Lometrexol hydrate
  • LY 264618 hydrate
  • 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 hydrate
  • Lometrexol(LY 264618)
  • L-Glutamic acid, N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-
  • 106400-81-1
  • Aromatics
  • Chiral Reagents
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals