2. Cell Cycle/DNA Damage Apoptosis
  3. Antifolate Apoptosis Caspase Bcl-2 Family
  4. Lometrexol hydrate

Lometrexol hydrate  (Synonyms: DDATHF hydrate)

Cat. No.: HY-14521B Purity: ≥99.0%
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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.

For research use only. We do not sell to patients.

Lometrexol hydrate Chemical Structure

Lometrexol hydrate Chemical Structure

CAS No. : 1435784-14-7

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Based on 1 publication(s) in Google Scholar

Other Forms of Lometrexol hydrate:

Lometrexol hydrate Related Antibodies

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1 Publications Citing Use of MCE Lometrexol hydrate

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Description

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[1][2][3].

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.

Lometrexol hydrate Related Antibodies

Cell Viability Assay[3]

Cell Line: Mouse leukemia L1210 cells
Concentration: 1, 30 μM
Incubation Time: 2, 4, 6, 8, 10 hours
Result: Induced rapid and complete growth inhibition.

Cell Cycle Analysis[3]

Cell Line: L1210 cells
Concentration: 1 μM
Incubation Time: 2, 4, 8, 12, 24 hours
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 (DDATHF; i.p.; 15-60 mg/kg; on gestation day 7.5) hydrate induces neural tube defects (NTDs) by disturbing purine metabolism and increases the rate of embryonic resorption and growth retardation in a dose-dependent manner[1].
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.

Animal Model: C57BL/6 mice (7-8 week, 18-20 g)[1]
Dosage: 15, 30, 35, 40, 45 and 60 mg/kg
Administration: Intraperitoneal injection; on gestation day 7.5
Result: Increased the rate of embryonic resorption and growth retardation in a dose-dependent manner.
Animal Model: C57BL/6 mice (7-8 week, 18-20 g)[1]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection; on gestation day 7.5
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.
Animal Model: C57BL/6 mice (7-8 week, 18-20 g)[1]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection; on gestation day 7.5, for 4 days
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.
Clinical Trial
Molecular Weight

461.47

Formula

C21H27N5O7
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1670 mL 10.8349 mL 21.6699 mL
5 mM 0.4334 mL 2.1670 mL 4.3340 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.20%

COA (246 KB)

Handling Instructions (2659 KB)
References

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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Lometrexol hydrate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lometrexol1435784-14-7DDATHFAntifolateApoptosisCaspaseBcl-2 FamilyantipurineantifolateGARFTnovopurinesynthesiscellproliferationapoptosiscyclearrestleukemiaL1210Inhibitorinhibitorinhibit

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