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| 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 | | EINECS: | | Product Categories: | Aromatics;Chiral Reagents;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals | | Mol File: | 106400-81-1.mol |
| 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 |
| Hazard Codes | T | | Risk Statements | 25 | | Safety Statements | 45 | | RIDADR | UN 2811 6.1 / PGIII | | WGK Germany | 3 |
| 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. |
| Lometrexol Preparation Products And Raw materials |
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