Lometrexol disodium
Based on 4 publication(s) in Google Scholar
Lometrexol (DDATHF) disodium, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol disodium can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol disodium has anticancer activity. Lometrexol disodium also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
For research use only. We do not sell to patients.
- Purity: 98.19%
- CAS No.: 120408-07-3
- Formula: C21H23N5Na2O6
- Molecular Weight:487.42
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Lometrexol disodium
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
All Caspase Isoforms
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Biological Activity
Lometrexol (DDATHF) disodium binds tightly to GART, resulting in a rapid and prolonged depletion of intracellular purine ribonucleotides[3].
Lometrexol (1-30 μM; 2-10 hours) disodium induces rapid and complete growth inhibition in L1210 cells[3].
Lometrexol (1 μM; 2-24 hours) disodium induces cell cycle arrest in murine leukemia L1210 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mouse leukemia L1210 cells
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Concentration:1, 30 μM
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Incubation Time:2, 4, 6, 8, 10 hours
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Result:Induced rapid and complete growth inhibition.
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Cell Line:L1210 cells
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Concentration:1 μM
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Incubation Time:2, 4, 8, 12, 24 hours
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Result:Caused a rapid loss of the G2/M phase population of cells and an early S phase accumulation of cells by 8 hours. By 24 h, the S phase population appeared to be slowly shifting to higher DNA content, and hence, from mid-to-late S phase.
Lometrexol (i.p.; 40 mg/kg; on gestation day 7.5) disodium decreases glycinamide ribonucleotide formyl transferase (GARFT) activity and Changes of ATP, GTP, dATP and dGTP levels[1].
Lometrexol (i.p.; 40 mg/kg; on gestation day 7.5) disodium induces abnormal proliferation and apoptosis exist in neural tube defects (NTDs)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (7-8 week, 18-20 g)[1]
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Dosage:15, 30, 35, 40, 45 and 60 mg/kg
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Administration:Intraperitoneal injection; on gestation day 7.5
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Result:Increased the rate of embryonic resorption and growth retardation in a dose-dependent manner.
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Animal Model:C57BL/6 mice (7-8 week, 18-20 g)[1]
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Dosage:40 mg/kg
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Administration:Intraperitoneal injection; on gestation day 7.5, for 0, 6, 24, 48 and 96 hours
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Result:Inhibited glycinamide ribonucleotide formyl transferase (GARFT) activity and GARFT activity was maximally inhibited after at 6 hours.
Decreased the levels of ATP, GTP, dATP, and dGTP of NTDs embryonic brain tissue significantly at 6 hours.
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Animal Model:C57BL/6 mice (7-8 week, 18-20 g)[1]
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Dosage:40 mg/kg
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Administration:Intraperitoneal injection; on gestation day 7.5, for 4 days
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Result:Decreased the expression of proliferation-related genes (Pcna, Foxg1 and Ptch1) and increased the expression of apoptosis-related genes (Bax, Casp8 and Casp9) in NTD groups.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 120408-07-3
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Appearance Solid
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Molecular Weight 487.42
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Formula C21H23N5Na2O6
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Color White to light yellow
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SMILES
O=C1C2=C(NC[C@H](CCC3=CC=C(C(N[C@@H](CCC(O[Na])=O)C(O[Na])=O)=O)C=C3)C2)N=C(N)N1
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Synonyms
DDATHF disodium
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (4)
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Journal Impact Factor
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Most Recent
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Nat Commun
Identification of purine biosynthesis as an NADH-sensing pathway to mediate energy stress. [Abstract]2022 Nov 17;13(1):7031. PMID: 36396642
Lometrexol disodium purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Nov 17;13(1):7031. [Abstract]
Effects of purine biosynthesis inhibitors on proliferation of HeLaTet-on EcSTH cells (n = 3 biologically independent samples). Cells were pretreated with the indicated inhibitors for 2 h and counted after treatment with Dox (1 µg/mL) and inhibitors for 48 h. 6-Mercaptopurine (6-MP, 300 µM), pelitrexol (PTrexol, 10 µM), Lometrexol (LTrexol, 10 µM).
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Sci Signal
Coordination between the eIF2 kinase GCN2 and p53 signaling supports purine metabolism and the progression of prostate cancer. [Abstract]2024 Nov 26;17(864):eadp1375. PMID: 39591412
Lometrexol disodium purchased from MedChemExpress. Usage Cited in: Sci Signal. 2024 Nov 26;17(864):eadp1375. [Abstract]
Measurements of cell death of 22Rv1 WT and GCN2 KO cells cultured in RPMI or MEM and treated with vehicle or Lometrexol (1 µM) for 6 days.
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Solvent & Solubility
H2O : 100 mg/mL (205.16 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Xu L, et, al. The effect of inhibiting glycinamide ribonucleotide formyl transferase on the development of neural tube in mice. Nutr Metab (Lond). 2016 Aug 23;13(1):56. [Content Brief]
[2]. Scaletti E, et, al. Structural basis of inhibition of the human serine hydroxymethyltransferase SHMT2 by antifolate drugs. FEBS Lett. 2019 Jul;593(14):1863-1873. [Content Brief]
[3]. Bronder JL, et, al. Antifolates targeting purine synthesis allow entry of tumor cells into S phase regardless of p53 function. Cancer Res. 2002 Sep 15;62(18):5236-41. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.0516 mL | 10.2581 mL | 20.5162 mL | 51.2905 mL |
| 5 mM | 0.4103 mL | 2.0516 mL | 4.1032 mL | 10.2581 mL | |
| 10 mM | 0.2052 mL | 1.0258 mL | 2.0516 mL | 5.1290 mL | |
| 15 mM | 0.1368 mL | 0.6839 mL | 1.3677 mL | 3.4194 mL | |
| 20 mM | 0.1026 mL | 0.5129 mL | 1.0258 mL | 2.5645 mL | |
| 25 mM | 0.0821 mL | 0.4103 mL | 0.8206 mL | 2.0516 mL | |
| 30 mM | 0.0684 mL | 0.3419 mL | 0.6839 mL | 1.7097 mL | |
| 40 mM | 0.0513 mL | 0.2565 mL | 0.5129 mL | 1.2823 mL | |
| 50 mM | 0.0410 mL | 0.2052 mL | 0.4103 mL | 1.0258 mL | |
| 60 mM | 0.0342 mL | 0.1710 mL | 0.3419 mL | 0.8548 mL | |
| 80 mM | 0.0256 mL | 0.1282 mL | 0.2565 mL | 0.6411 mL | |
| 100 mM | 0.0205 mL | 0.1026 mL | 0.2052 mL | 0.5129 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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