Trimelamol
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].
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- No. CAS: 64124-21-6
- Fòrmula: C9H18N6O3
- Peso molecular:258.28
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Almacenamiento:
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Actividad biológica
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Chemical Information
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| GCT | IC50 |
24.3 μM
Compound: 1
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In vitro cytotoxicity against GCT cell lines
In vitro cytotoxicity against GCT cell lines
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[PMID: 8277501] |
| L1210 | IC50 |
33.4 μM
Compound: 1
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In vitro cytotoxicity against L1210 murine lymphocytic leukemia cell lines
In vitro cytotoxicity against L1210 murine lymphocytic leukemia cell lines
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[PMID: 8277501] |
| NCI-H69 | IC50 |
8.5 μM
Compound: 1
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In vitro cytotoxicity against human small cell lung cancer H69 cell lines
In vitro cytotoxicity against human small cell lung cancer H69 cell lines
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[PMID: 8277501] |
| PC-6 | IC50 |
12.9 μM
Compound: 1
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In vitro cytotoxicity against PC6 murine plasmacytoma cell lines
In vitro cytotoxicity against PC6 murine plasmacytoma cell lines
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[PMID: 8277501] |
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.
| Species | Dose | Route | Plasma Concentration | Brain Concentration |
|---|---|---|---|---|
| Mice | 90 mg/kg | i.p. | 33.8 μg/mL | 0.54 mL/mg/kg |
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.
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Animal Model:(PXN/65, HX110, HX110P, HX62, T-61) xenograft tumor model in nude mice[4]
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Dosage:15 mg/kg, 30 mg/kg, 60 mg/kg for PXN/65, HX110, HX110P, HX62; 15 mg/kg for T-61
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Administration:Intraperitoneal injection (i.p.), once a day for 5 days, 4 consecutive weeks
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Result:had curative activity against PXN/65, HX110, HX110P, and T-61, but HX62 was non-curative but had a better T/C value (0.20) than cisplatin (0.40–0.84).
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Animal Model:(T-61, MX-1, Br-10, R-27, MCF-7) xenograft tumor model in BALB/c famale mice(6-7 weeks, 20-22 g)[5]
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Dosage:60 mg/kg, 30 mg/kg, 15 mg/kg, 7.5 mg/kg for T-61, MX-1; 60 mg/kg for Br-10, R-27, MCF-7
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Administration:Intraperitoneal injection (i.p.), once a day for 5 days, 3 consecutive weeks
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Result:Completely regressed tumors in the T-61 model at 60 mg/kg. Significantly reduced tumor weight at 30 mg/kg (T/C = 3.8%).
Completely regressed tumors in the MX-1 model at both 60 and 30 mg/kg. Reduced tumor weight at 15 mg/kg (T/C = 8.3%).
Exhibited marginal activity in the Br-10 model at 60 mg/kg (T/C = 48.2%). Was insensitive in the R-27 and MCF-7 tumor models.
Chemical Information
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No. CAS 64124-21-6
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Peso molecular 258.28
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Fòrmula C9H18N6O3
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SMILES
OCN(C1=NC(N(C)CO)=NC(N(C)CO)=N1)C
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Synonyms
CB 10-375; NSC 283162
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Trimelamol Related Classifications
HY-106768 Related Classifications
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