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Lometrexol (hydrate)

CAT: 0804-HY-14521B-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-14521B-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) 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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
Phase 2

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