Lometrexol disodium

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MedKoo CAT#: 205977

CAS#: 120408-07-3 (sodium)

Description: Lometrexol is a folate analog antimetabolite with antineoplastic activity. As the 6R diastereomer of 5,10-dideazatetrahydrofolate, lometrexol inhibits glycinamide ribonucleotide formyltransferase (GARFT), the enzyme that catalyzes the first step in the de novo purine biosynthetic pathway, thereby inhibiting DNA synthesis, arresting cells in the S phase of the cell cycle, and inhibiting tumor cell proliferation. The agent has been shown to be active against tumors that are resistant to the folate antagonist methotrexate.

Price and Availability

Size Price Shipping out time Quantity
5mg USD 250 2 Weeks
10mg USD 450 2 Weeks
25mg USD 750 2 Weeks
50mg USD 1250 2 Weeks
100mg USD 1950 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-31. Prices are subject to change without notice.

Lometrexol disodium, purity > 98%, is in stock. The same day shipping out after order is received. Note: Bulk quantity is available via custom synthesis. The lead time is about 2 months. Please send email to sales@medkoo.com for quotation of bulk quantities.

Chemical Structure


Theoretical Analysis

MedKoo Cat#: 205977
Name: Lometrexol disodium
CAS#: 120408-07-3 (sodium)
Chemical Formula: C21H23N5Na2O6
Exact Mass:
Molecular Weight: 487.42
Elemental Analysis: C, 51.75; H, 4.76; N, 14.37; Na, 9.43; O, 19.69

Related CAS #: 120408-07-3 (sodium)   106400-81-1 (free acid)    

Synonym: LY 264618; LY-264618; LY264618; NSC722969; NSC-722969; NSC-722969. (6R)DDATHF; LMTX; DDATHF disodium; Lometrexol sodium; Lometrexol.

IUPAC/Chemical Name: Disodium (4-(2-((R)-2-amino-4-oxo-1,4,5,6,7,8-hexahydropyrido[2,3-d]pyrimidin-6-yl)ethyl)benzoyl)-L-glutamate


InChi Code: InChI=1S/C21H25N5O6.2Na/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);;/q;2*+1/p-2/t12-,15+;;/m1../s1

SMILES Code: O=C(O[Na])[C@@H](NC(C1=CC=C(CC[C@@H](CN2)CC3=C2NC(N)=NC3=O)C=C1)=O)CCC(O[Na])=O

Technical Data

White to off-white solid powder

>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (SDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Soluble in DMSO, soluble in water.

Shelf Life:
>5 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:

Additional Information

 Related CAS#: 120408-07-3 (Lometrexol disodium); 106400-81-1 (Lometrexol)

Lometrexol free acid:
Chemical Formula: C21H25N5O6
Exact Mass: 443.1805
Molecular Weight: 443.4600
Elemental Analysis: C, 56.88; H, 5.68; N, 15.79; O, 21.65


1: Roberts JD, Poplin EA, Tombes MB, Kyle B, Spicer DV, Grant S, Synold T, Moran R. Weekly lometrexol with daily oral folic acid is appropriate for phase II evaluation. Cancer Chemother Pharmacol. 2000;45(2):103-10. PubMed PMID: 10663624.

2: Synold TW, Newman EM, Carroll M, Muggia FM, Groshen S, Johnson K, Doroshow JH. Cellular but not plasma pharmacokinetics of lometrexol correlate with the occurrence of cumulative hematological toxicity. Clin Cancer Res. 1998 Oct;4(10):2349-55. PubMed PMID: 9796964.

3: Habeck LL, Chay SH, Pohland RC, Worzalla JF, Shih C, Mendelsohn LG. Whole-body disposition and polyglutamate distribution of the GAR formyltransferase inhibitors LY309887 and lometrexol in mice: effect of low-folate diet. Cancer Chemother Pharmacol. 1998;41(3):201-9. PubMed PMID: 9443636.

4: Turner RN, Aherne GW, Curtin NJ. Selective potentiation of lometrexol growth inhibition by dipyridamole through cell-specific inhibition of hypoxanthine salvage. Br J Cancer. 1997;76(10):1300-7. PubMed PMID: 9374375; PubMed Central PMCID: PMC2228144.

5: Muggia FM, Synold TW, Newman EM, Jeffers S, Leichman LP, Doroshow JH, Johnson K, Groshen S. Failure of pretreatment with intravenous folic acid to alter the cumulative hematologic toxicity of lometrexol. J Natl Cancer Inst. 1996 Oct 16;88(20):1495-6. PubMed PMID: 8841028.

6: Synold TW, Xi B, Newman EM, Muggia FM, Doroshow JH. Simple and sensitive method for the quantitative analysis of lometrexol in plasma using high-performance liquid chromatography with electrochemical detection. J Chromatogr B Biomed Appl. 1996 Aug 30;683(2):245-9. PubMed PMID: 8891922.

7: Sessa C, de Jong J, D'Incalci M, Hatty S, Pagani O, Cavalli F. Phase I study of the antipurine antifolate lometrexol (DDATHF) with folinic acid rescue. Clin Cancer Res. 1996 Jul;2(7):1123-7. PubMed PMID: 9816277.

8: Alati T, Worzalla JF, Shih C, Bewley JR, Lewis S, Moran RG, Grindey GB. Augmentation of the therapeutic activity of lometrexol -(6-R)5,10-dideazatetrahydrofolate- by oral folic acid. Cancer Res. 1996 May 15;56(10):2331-5. PubMed PMID: 8625328.