Lometrexol

• UNSPSC Description:

  Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor[1][2][3].

• Target Antigen:

  Antifolate; Apoptosis; Bcl-2 Family; Caspase

• Type:

  Reference compound

• Related Pathways:

  Apoptosis;Cell Cycle/DNA Damage

• Applications:

  Neuroscience-Neurodegeneration

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/LY_264618.html

• Solubility:

  DMSO : 100 mg/mL (ultrasonic)

• Smiles:

  O=C1C2=C(NC[C@H](CCC3=CC=C(C(N[C@@H](CCC(O)=O)C(O)=O)=O)C=C3)C2)N=C(N)N1

• Molecular Weight:

  443.45

• 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.

• Shipping Conditions:

  Room Temperature

• Clinical Information:

  Phase 2

• CAS Number:

  106400-81-1