| ln Vitro |
DMAPT-DTCs-1,3-diaminopropane-DTCs-DMAPT dimethylsulfonate (compound 92) showed selective antiproliferative activity against NCI-H820 lung adenocarcinoma cells (IC50 = 0.86 μM) but reduced efficacy against normal 3T3 fibroblasts (IC50 = 1.83 μM) [1].
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| ln Vivo |
DMAPT-DTCs-1,3-diaminopropane-DTCs-DMAPT dimethylsulfonate (compound 92) (20-50 mg/kg; intraperitoneal injection; once every 2 days for 19 days) showed potent anti-lung cancer activity in the NCI-H820 CDX model, reducing tumor volume and weight, and inducing apoptosis, ferroptosis and copper death [1]. DMAPT-DTCs-1,3-diaminopropane-DTCs-DMAPT dimethylsulfonate (20-100 mg/kg; oral or intraperitoneal injection; once every 2 days for 17 days) showed anti-lung cancer activity in the lung adenocarcinoma PDX model by inducing apoptosis, ferroptosis and copper death [1]. DMAPT-DTCs-1,3-diaminopropane-DTCs-DMAPT dimethylsulfonate (20-500 mg/kg; oral, intraperitoneal; single dose) showed no significant in vivo toxicity at oral doses up to 500 mg/kg and intraperitoneal doses up to 50 mg/kg, with only mild toxicity observed at an intraperitoneal dose of 100 mg/kg [1].
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| Animal Protocol |
Animal/Disease Models:Balb/c mice (female, n=7 per group; subcutaneously inoculated with 5 × 10⁶ NCI-H820 cells) [1]
Doses: 20 mg/kg; 50 mg/kg Route of Administration: Intraperitoneal injection; once every 2 days; for 19 days Experimental Results: Compared with the control group, tumor volume and tumor weight were significantly reduced without affecting mouse body weight. The levels of anti-apoptotic protein Bcl-2, ferroptosis-related protein GPX4, and copper death-related proteins FDX1 and DLAT in tumor tissue were significantly reduced. The level of pro-apoptotic protein Bax was significantly increased. Animal/Disease Models:Balb/c nude mice (n=6 per group; subcutaneous inoculation with 3-5 mm³ patient-derived lung adenocarcinoma tissue) [1] Doses: 50 mg/kg (oral); 100 mg/kg (oral); 20 mg/kg (intraperitoneal); 50 mg/kg (intraperitoneal) Route of Administration: Oral; every 2 days for 17 days; Intraperitoneal; every 2 days for 17 days Experimental Results: Compared with the control group, all tested doses reduced tumor volume and tumor weight without affecting mouse body weight. The levels of anti-apoptotic protein Bcl-2, ferroptosis-related protein GPX4, and copper death-related proteins FDX1 and DLAT in tumor tissue were significantly reduced. The level of pro-apoptotic protein Bax was significantly increased. Intraperitoneal administration showed better efficacy compared with oral administration. |
| References |
| Appearance |
Typically exists as solids at room temperature
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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.) |
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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