Lometrexol (hydrate)

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].

Product Specifications

CAS Number

[1435784-14-7]

Product Name Alternative

DDATHF (hydrate)

UNSPSC

12352005

Target

Antifolate; Apoptosis; Bcl-2 Family; Caspase

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/lometrexol-hydrate.html

Purity

99.20

Solubility

DMSO : 40 mg/mL (ultrasonic; warming)

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

Molecular Formula

C21H27N5O7

Molecular Weight

461.47

References & Citations

[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.|[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.|[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.