Lometrexol hydrate

≥95% (HPLC)

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, LY 264618 hydrate
Empirical Formula (Hill Notation):
C21H25N5O6 · xH2O
Número de CAS:
Peso molecular:
443.45 (anhydrous basis)
PubChem Substance ID:
En este momento no podemos mostrarle ni los precios ni la disponibilidad

Quality Level


≥95% (HPLC)




white to light yellow


DMSO: ≥5 mg/mL

storage temp.


SMILES string




InChI key



Lometrexol hydrate was used to compare the biological activity of potent inhibitor of human GARFTase.


5, 25 mg in glass bottle

Biochem/physiol Actions

Glycinamide Ribonucleotide Formyltransferase (GARFTase) is a folate-dependent enzyme required for de novo purine synthesis. Lometrexate is a potent inhibitor of GARFTase, but does not interfere with enzymes involved in the synthesis of folate. Lometrexerol has been tested clinically for the treatment of various cancers as an anti-folate like agent, similar to methotrexate. Treatment with lometrexol rapidly decreases ATP and GTP levels, cell cycle arrest and induces apoptosis. Although depletion of nucleotide pools induces p53 expression, lometrexol is cytotoxic in both wild-type and mutant p53 expressing tumor cells. Lometrexol is cytotoxic in CCRF-CEm leukemia cells with an IC50 of 2.9 nM.


Skull and crossbones





UN 2811 6.1 / PGIII

WGK Germany


Flash Point F

Not applicable

Flash Point C

Not applicable

New agents in cancer clinical trials.
J Adams et al.
Oncogene, 19(56), 6687-6692 (2001-06-28)
D R Newell
Seminars in oncology, 26(2 Suppl 6), 74-81 (1999-12-22)
Antifolate drugs, as a class, have broad-spectrum activity against both hematologic and solid human malignancies. The pharmacokinetics of the classical antifolate methotrexate have been well-defined and pharmacokinetic data can be exploited to reduce the toxicity and enhance the activity of...
C Shih et al.
Advances in enzyme regulation, 38, 135-152 (1998-10-08)
Extensive biochemical and pharmacological evidence indicates that LY231514 is a novel antifolate antimetabolite. LY231514 is transported into cells mainly through the reduced folate carrier system and extensively metabolized to polyglutamated forms. The polyglutamates of LY231514 inhibit at least three key...
G Jansen et al.
The Journal of biological chemistry, 273(46), 30189-30198 (1998-11-07)
CEM/MTX is a subline of human CCRF-CEM leukemia cells which displays >200-fold resistance to methotrexate (MTX) due to defective transport via the reduced folate carrier (RFC). CEM/MTX-low folate (LF) cells, derived by a gradual deprivation of folic acid from 2.3...
J I Borrell et al.
Journal of medicinal chemistry, 44(14), 2366-2369 (2001-06-29)
We recently described the syntheses of 12a-c, 4-amino-7-oxo substituted analogues of 5-deaza-5,6,7,8-tetrahydrofolic acid (5-DATHF), and 5,10-dideaza-5,6,7,8-tetrahydrofolic acid (DDATHF), in six steps from commercially available p-substituted methyl benzoates in 20-27% overall yields. Such analogues were tested in vitro against CCRF-CEM leukemia...

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