Lometrexol hydrate
Based on 7 publication(s) in Google Scholar
Lometrexol (DDATHF) hydrate, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
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- Pureza : 98.96%
- No. CAS: 1435784-14-7
- Fòrmula: C21H27N5O7
- Peso molecular:461.47
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Almacenamiento:
4°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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Actividad biológica
Descripciòn
In Vitro
Lometrexol (DDATHF) hydrate binds tightly to GART, resulting in a rapid and prolonged depletion of intracellular purine ribonucleotides[3].
Lometrexol (1-30 μM; 2-10 hours) hydrate induces rapid and complete growth inhibition in L1210 cells[3].
Lometrexol (1 μM; 2-24 hours) hydrate 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.
In Vivo
Lometrexol (i.p.; 40 mg/kg; on gestation day 7.5) hydrate 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) hydrate 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
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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.
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- PCNA Immunodetection Proliferation Assay
- Flow cytometric DNA-content cell-cycle staining
- Protocol for Cell Counting and Cell Density Analysis
- Apoptosis Solutions
- MTT Cell Proliferation Assay
Chemical Information
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No. CAS 1435784-14-7
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Appearance Solid
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Peso molecular 461.47
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Fòrmula C21H27N5O7
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Color White to off-white
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SMILES
O=C(O)CC[C@@H](C(O)=O)NC(C1=CC=C(CC[C@@H](CN2)CC3=C2N=C(N)NC3=O)C=C1)=O.O
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Synonyms
DDATHF hydrate
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (7)
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Journal Impact Factor
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Most Recent
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Nature
2026 Jul;655(8125):1300-1308. PMID: 42457960 -
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 hydrate 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 hydrate 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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Solvente y solubilidad
In Vitro:
DMSO : 40 mg/mL (86.68 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (276 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)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1670 mL | 10.8349 mL | 21.6699 mL | 54.1747 mL |
| 5 mM | 0.4334 mL | 2.1670 mL | 4.3340 mL | 10.8349 mL | |
| 10 mM | 0.2167 mL | 1.0835 mL | 2.1670 mL | 5.4175 mL | |
| 15 mM | 0.1445 mL | 0.7223 mL | 1.4447 mL | 3.6116 mL | |
| 20 mM | 0.1083 mL | 0.5417 mL | 1.0835 mL | 2.7087 mL | |
| 25 mM | 0.0867 mL | 0.4334 mL | 0.8668 mL | 2.1670 mL | |
| 30 mM | 0.0722 mL | 0.3612 mL | 0.7223 mL | 1.8058 mL | |
| 40 mM | 0.0542 mL | 0.2709 mL | 0.5417 mL | 1.3544 mL | |
| 50 mM | 0.0433 mL | 0.2167 mL | 0.4334 mL | 1.0835 mL | |
| 60 mM | 0.0361 mL | 0.1806 mL | 0.3612 mL | 0.9029 mL | |
| 80 mM | 0.0271 mL | 0.1354 mL | 0.2709 mL | 0.6772 mL |
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