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ChemicalBook >> CAS DataBase List >>Lometrexol

Lometrexol

CAS No.
106400-81-1
Chemical Name:
Lometrexol
Synonyms
Lometrexol hydrate;LY 264618;Lometrexol;Lometrexolum;LY 264618 hydrate;Lometrexol(LY 264618);Lometrexolum [inn-latin];Lometrexol, 10 mM in DMSO;(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
CBNumber:
CB81179064
Molecular Formula:
C21H25N5O6
Molecular Weight:
443.45
MDL Number:
MOL File:
106400-81-1.mol
MSDS File:
SDS
TDS File:
TDS
Last updated:2026-05-28 03:03:37
Product description Number Pack Size Price
Lometrexol hydrate ≥95% (HPLC) SML0040 5mg $294
Lometrexol hydrate ≥95% (HPLC) SML0040 25mg $1220
Lometrexol (hydrate) ≥98% 18049 1mg $107
Lometrexol (hydrate) ≥98% 18049 5mg $268
Lometrexol ≥98% 18049 1mg $97

Lometrexol 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
InChIKey AEFQSKJUVDZANQ-YLCXCWDSSA-N
SMILES O.NC1=NC(=O)C2=C(NC[C@H](CCc3ccc(cc3)C(=O)N[C@@H](CCC(O)=O)C(O)=O)C2)N1
NCI Dictionary of Cancer Terms lometrexol
FDA UNII 6P3AVY8A7Q
NCI Drug Dictionary lometrexol
UNSPSC Code 12352200
NACRES NA.77

SAFETY

Risk and Safety Statements

Symbol(GHS)  Skull and Crossbones (GHS06)
GHS06
Signal word  Danger
Hazard statements  H301
Precautionary statements  P301+P310
Hazard Codes  T
Risk Statements  25
Safety Statements  45
RIDADR  UN 2811 6.1 / PGIII
WGK Germany  3
Storage Class 6.1C - Combustible acute toxic Cat.3
toxic compounds or compounds which causing chronic effects
Hazard Classifications Acute Tox. 3 Oral

Lometrexol price More Price(31)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich SML0040 Lometrexol hydrate ≥95% (HPLC) 106400-81-1 5mg $294 2026-04-30 Buy
Sigma-Aldrich SML0040 Lometrexol hydrate ≥95% (HPLC) 106400-81-1 25mg $1220 2026-04-30 Buy
Cayman Chemical 18049 Lometrexol (hydrate) ≥98% 1mg $107 2026-04-30 Buy
Cayman Chemical 18049 Lometrexol (hydrate) ≥98% 5mg $268 2026-04-30 Buy
Cayman Chemical 18049 Lometrexol ≥98% 106400-81-1 1mg $97 2024-03-01 Buy
Product number Packaging Price Buy
SML0040 5mg $294 Buy
SML0040 25mg $1220 Buy
18049 1mg $107 Buy
18049 5mg $268 Buy
18049 1mg $97 Buy

Lometrexol Chemical Properties,Uses,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

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

Uses

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

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.

References

[1] G P BEARDSLEY. A new folate antimetabolite, 5,10-dideaza-5,6,7,8-tetrahydrofolate is a potent inhibitor of de novo purine synthesis.[J]. The Journal of Biological Chemistry, 1989, 264 1: 328-333.
[2] G PIZZORNO. (6R)-5,10-Dideaza-5,6,7,8-tetrahydrofolic acid effects on nucleotide metabolism in CCRF-CEM human T-lymphoblast leukemia cells.[J]. Cancer research, 1991, 51 9: 2291-2295.
[3] JULIE L BRONDER  Richard G M. Antifolates targeting purine synthesis allow entry of tumor cells into S phase regardless of p53 function.[J]. Cancer research, 2002, 62 18: 5236-5241.

Lometrexol Preparation Products And Raw materials

Raw materials

Preparation Products

Lometrexol Suppliers

Global( 42)Suppliers
Supplier Tel Email Country ProdList Advantage
TargetMol Chemicals Inc.
+1-781-999-5354; +17819995354 marketing@targetmol.com United States 32466 58
Aladdin Scientific
tp@aladdinsci.com United States 52923 58
J & K SCIENTIFIC LTD. 18210857532; 18210857532 jkinfo@jkchemical.com China 96815 76
LGM Pharma 1-(800)-881-8210 inquiries@lgmpharma.com United States 2123 70
Chemsky (shanghai) International Co.,Ltd 021-50135380 shchemsky@sina.com China 15402 60
BOC Sciences 1-631-485-4226; 16314854226 info@bocsci.com United States 9920 65
Sigma-Aldrich 021-61415566 800-8193336 orderCN@merckgroup.com China 51395 80
Shanghai YuanYe Biotechnology Co., Ltd. 021-61312847; 18021002903 3008007409@qq.com China 89686 60
Beijing Jin Ming Biotechnology Co., Ltd. 010-60605840 18892239720 psaitong@jm-bio.com China 12306 58
Shenzhen Polymeri Biochemical Technology Co., Ltd. +86-400-002-6226 +86-13028896684; sales@rrkchem.com China 57422 58

Lometrexol Spectrum

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 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]- Lometrexol, 10 mM in DMSO Lometrexol hydrate 106400-81-1 Aromatics Chiral Reagents Heterocycles Intermediates & Fine Chemicals Pharmaceuticals
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