Lometrexol disodium (Synonyms: DDATHF disodium)

Name: Lometrexol disodium
Brand: MedChemExpress
SKU: HY-14521A
Rating: 4.5 (1 reviews)

Cat. No.: HY-14521A Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

Lometrexol disodium Chemical Structure

CAS No. : 120408-07-3

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Other Forms of Lometrexol disodium:

LY243246 Get quote
Lometrexol Get quote
Lometrexol hydrate Get quote

1 Publications Citing Use of MCE Lometrexol disodium

•Nat Commun. 2022 Nov 17;13(1):7031. [Abstract]

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Biological Activity
Purity & Documentation
References
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Description

In Vitro

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.

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) disodium 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) 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.

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, for 0, 6, 24, 48 and 96 hours
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

487.42

Formula

C₂₁H₂₃N₅Na₂O₆

CAS No.

120408-07-3

Appearance

Solid

Color

White to light yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°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:

H₂O : 100 mg/mL (205.16 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0516 mL	10.2581 mL	20.5162 mL
5 mM	0.4103 mL	2.0516 mL	4.1032 mL
10 mM	0.2052 mL	1.0258 mL	2.0516 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.

* 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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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

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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)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: ≥98.0%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (248 KB)

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

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.

Lometrexol disodium 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.

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Lometrexol disodium (Synonyms: DDATHF disodium)

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Other Forms of Lometrexol disodium:

Lometrexol disodium Related Antibodies

1 Publications Citing Use of MCE Lometrexol disodium

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Lometrexol disodium Related Antibodies

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Complete Stock Solution Preparation Table

Lometrexol disodium Related Classifications

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