Trimelamol  (Synonyms: CB 10-375; NSC 283162)

Trimelamol (CB10-375; NSC283162) is a highly efficient acid-catalyzed DNA interstrand crosslinker with low neurotoxicity due to its limited BBB penetration. Trimelamol exhibits anti-tumor activity and overcomes platinum resistance. Trimelamol is investigated for lung and ovarian cancer research^{[1][2][3][4][5]}.

Trimelamol exerts its cytotoxicity directly through its N-hydroxymethyl group, and the toxicity is irreversible after the drug is removed. It has a faster onset of action than HMM and PMM^[1][2].

Trimelamol (0.5-500 μM, 1 h) cross-linking is its main anti-tumor mechanism. In ³²P-end-labelled pBR322 plasmid DNA, it significantly cross-links DNA at concentrations ≥ 2.5 μM, and the cross-linking efficiency is higher under acidic conditions^[3].

Trimelamol has a broad spectrum of cytotoxicity and is effective against platinum-resistant ovarian cancer cells (IC₅₀ range: 8.5-55.4 μM)^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Trimelamol (15-60 mg/kg, i.p., once a day for 5 days, 4 consecutive weeks) is effective against platinum-sensitive/resistant ovarian cancer and hormone-dependent breast cancer in xenograft model mice, especially in the acquired resistance model^[4].

Trimelamol (7.5-60 mg/kg, i.p, once a day for 5 days, 3 consecutive weeks) administered parenterally was significantly effective in BALB/c female mice bearing subcutaneous T-61/MX-1 tumors and less active in BALB/c female mice bearing subcutaneous Br-10 tumors. It exhibited moderate toxicity at high doses, but manageable toxicity at low concentrations^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

258.28

C₉H₁₈N₆O₃

64124-21-6

OCN(C1=NC(N(C)CO)=NC(N(C)CO)=N1)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. I R Judson, et al. Phase I trial and pharmacokinetics of trimelamol (N2,N4,N6-trihydroxymethyl-N2,N4,N6-trimethylmelamine). Cancer Res. 1989 Oct 1;49(19):5475-9.  [Content Brief]

  [2]. I R Judson, et al. Low central nervous system penetration of N2,N4,N6,-trihydroxymethyl-N2,N4,N6,-trimethylmelamine (Trimelamol): a cytotoxic s-triazine with reduced neurotoxicity. Br J Cancer. 1986 May;53(5):601-6.  [Content Brief]

  [3]. C Jackson, et al. N2,N4,N6-tri(hydroxymethyl)-N2,N4,N6-trimethylmelamine (trimelamol) is an efficient DNA cross-linking agent in vitro. Biochem Pharmacol. 1991 Nov 6;42(11):2091-7.  [Content Brief]

  [4]. H M Coley, et al. Pre-clinical development of the anti-tumour agent CB 7646, bis N-(hydroxymethyl) trimethylmelamine, a stable analogue of trimelamol. Int J Cancer. 1996 Nov 4;68(3):356-63.  [Content Brief]

  [5]. Y Yamada, et al. Antitumor effect of trimelamol against human breast carcinoma xenografts in nude mice. Oncol Rep. 1996 Jul;3(4):613-7.  [Content Brief]