| Size | Price | Stock | Qty |
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| 250mg |
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| ln Vitro |
Trimelamor exerts its cytotoxicity directly through its N-hydroxymethyl group, and the toxicity is irreversible after drug removal. Its onset of action is faster than that of HMM and PMM[1][2]. Cross-linking of trimeramol (0.5-500 μM, 1 h) is its main antitumor mechanism. In pBR322 plasmid DNA labeled with 32P ends, trimeramol can significantly cross-link DNA at concentrations ≥2.5 μM, and the cross-linking efficiency is higher under acidic conditions[3]. Trimelamor has broad-spectrum cytotoxicity and is effective against platinum-resistant ovarian cancer cells (IC50 range: 8.5-55.4 μM)[4].
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| ln Vivo |
In xenograft mouse models, trimeramol (15-60 mg/kg, intraperitoneal injection, once daily for 5 days for 4 weeks) was effective against platinum-sensitive/resistant ovarian cancer and hormone-dependent breast cancer, especially in acquired resistance models [4]. In BALB/c female mice carrying subcutaneous T-61/MX-1 tumors, parenteral administration of trimeramol (7.5-60 mg/kg, intraperitoneal injection, once daily for 5 days for 3 weeks) was significantly effective, but less effective in BALB/c female mice carrying subcutaneous Br-10 tumors. High doses had moderate toxicity, while low concentrations had manageable toxicity [5].
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| Animal Protocol |
Animal/Disease Models:(PXN/65, HX110, HX110P, HX62, T-61) nude mouse xenograft tumor model [4]
Doses: The doses of PXN/65, HX110, HX110P, and HX62 were 15 mg/kg, 30 mg/kg, and 60 mg/kg, respectively; the dose of T-61 was 15 mg/kg. Route of Administration: Intraperitoneal injection (ip), once daily for 5 consecutive days for 4 weeks. Experimental Results: It has curative activity against PXN/65, HX110, HX110P, and T-61, but no curative effect on HX62. However, its T/C value (0.20) is better than that of cisplatin (0.40–0.84). Animal/Disease Models:BALB/c female mouse xenograft tumor model (T-61, MX-1, Br-10, R-27, MCF-7) (6-7 weeks old, 20-22 g) [5] Doses: T-61, MX-1: 60 mg/kg, 30 mg/kg, 15 mg/kg, 7.5 mg/kg; Br-10, R-27, MCF-7: 60 mg/kg Route of Administration: Intraperitoneal injection (ip), once daily for 5 consecutive days for 3 weeks Experimental Results: At a dose of 60 mg/kg, the tumors in the T-61 model completely regressed. At a dose of 30 mg/kg, the tumor weight was significantly reduced (T/C = 3.8%). In the MX-1 model, the tumors completely regressed at doses of 60 mg/kg and 30 mg/kg. At a dose of 15 mg/kg, tumor weight was reduced (T/C = 8.3%). In the Br-10 model, the activity was weaker at a dose of 60 mg/kg (T/C = 48.2%). The drug was ineffective in the R-27 and MCF-7 tumor models. |
| References |
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| Molecular Formula |
C9H18N6O3
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|---|---|
| Molecular Weight |
258.28
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| CAS # |
64124-21-6
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| Appearance |
Typically exists as solids at room temperature
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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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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8718 mL | 19.3588 mL | 38.7177 mL | |
| 5 mM | 0.7744 mL | 3.8718 mL | 7.7435 mL | |
| 10 mM | 0.3872 mL | 1.9359 mL | 3.8718 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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