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Lometrexol

CAT: 0804-HY-14521-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-14521-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
CAS Number
106400-81-1
Product Name Alternative
DDATHF
UNSPSC
12352005
Hazard Statement
H301
Target
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
Purity
98.96
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 Formula
C21H25N5O6
Molecular Weight
443.45
Precautions
H301
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
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2

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