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: 98.96%
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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.

CAS No. : 1435784-14-7

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Based on 4 publication(s) in Google Scholar

Other Forms of Lometrexol hydrate:

Lometrexol hydrate Related Antibodies

Top Publications Citing Use of Products

    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.

    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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    Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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    • Customer Review

    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.
    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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    This equation is commonly abbreviated as: C1V1 = C2V2

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

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

    Purity: 99.20%

    SDS (252 KB)

    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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