A GART inhibitor
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Lometrexol (hydrate)

Item No. 18049

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid, hydrate
Synonyms
  • DDATHF
  • (6R)-Dideazatetrahydrofolate
Molecular Formula
C21H25N5O6 • XH2O
Formula Weight
443.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 20 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/ml
λmax
224, 279 nm
SMILES
O=C(N[C@H](C(O)=O)CCC(O)=O)C1=CC=C(CC[C@H]2CNC(N=C(N)NC3=O)=C3C2)C=C1
InChi Code
InChI=1S/C21H25N5O6/c22-21-25-17-14(19(30)26-21)9-12(10-23-17)2-1-11-3-5-13(6-4-11)18(29)24-15(20(31)32)7-8-16(27)28/h3-6,12,15H,1-2,7-10H2,(H,24,29)(H,27,28)(H,31,32)(H4,22,23,25,26,30)/t12-,15+/m1/s1
InChi Key
ZUQBAQVRAURMCL-DOMZBBRYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $107

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    5 mg

    $268

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    Cayman Chemical
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    Product Description

    Lometrexol is a folate analog antimetabolite with antineoplastic activity.1,2 At nanomolar conentrations, it inhibits GART preventing de novo purine synthesis, inhibiting DNA synthesis, arresting cells in the S phase of the cell cycle, and inhibiting tumor cell proliferation.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Beardsley, G.P., Moroson, B.A., Taylor, E.C., et al. A new folate antimetabolite, 5,10-dideaza-5,6,7,8-tetrahydrofolate is a potent inhibitor of de novo purine synthesis. The Journal of Biological Chemisty 264(1), 328-333 (1989).

    2. Pizzorno, G., Moroson, B.A., Cashmore, A.R., et al. (6R)-5,10-Dideaza-5,6,7,8-tetrahydrofolic acid effects on nucleotide metabolism in CCRF-CEM human T-lymphoblast leukemia cells. Cancer Res. 51(9), 2291-2295 (1991).

    3. Bronder, J.L., and Moran, R.G. Antifolates targeting purine synthesis allow entry of tumor cells into S phase regardless of p53 function. Cancer Res. 62(18), 5236-5241 (2002).