| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Anticancer agent 205 (compound 9) (4 µM; 1 h) interacts with G4-mtDNA in HCT116 cells[1]. Anticancer agent 205 (0, 1, 2, 4 µM; 48 h) reduces the mRNA levels of ND2 and ND5 in HCT116 and HFF1 cells[1]. Anticancer agent 205 (0, 1, 2, 4 µM; 48 h) reduces the protein levels of ND3, ND4, ND6, COX1, COX2, COX3, CYTB, ATP6, and ATP8 in HCT116 cells[1]. Anticancer agent 205 (0-4 µM) increases ROS levels in a concentration-dependent manner[1]. Anticancer agent 205 (0-4 µM; 72 h) induces DNA damage and cell senescence[1].
|
|---|---|
| ln Vivo |
Anticancer agent 205 (5 mg/kg; iv; every 2 days for 16 days) inhibits tumor growth in the HCT116 xenograft mouse model [1].
|
| Cell Assay |
Cell Cytotoxicity Assay[1]
Cell Types: HCT116, LoVo, HeLa, HepG2, PANC-1, MDA-MB-231, HFF1, BJ Tested Concentrations: 0-40 µM Incubation Duration: 48 h Experimental Results: Showed cytotoxicity for HCT116, LoVo, HeLa, HepG2, PANC-1, MDA-MB-231, HFF1, BJ cells with IC50s of 3.4, 13.4, 23.5, >40, 24.8, 34.6, 32.7, >40 µM, respectively. Western Blot Analysis[1] Cell Types: HCT116 Tested Concentrations: 0, 1, 2, 4 µM Incubation Duration: 48 h Experimental Results: Showed that the protein levels of ND3, ND4, ND6, COX1, COX2, COX3, CYTB, ATP6, and ATP8 were decreased markedly. RT-PCR[1] Cell Types: HCT116, HFF1 Tested Concentrations: 0, 1, 2, 4 µM Incubation Duration: 48 h Experimental Results: Caused a significant reduction of mRNA levels for ND1, ND2, ND3, ND4, ND4L, ND5, COX2, ATP6, and ATP8 in HCT116, only ND2 and ND5 showed a significant reduction in HFF1 cells. Cell Cycle Analysis[1] Cell Types: HCT116 Tested Concentrations: 0, 1, 2, 4 µM Incubation Duration: 48 h Experimental Results: Induced cell cycle arrested in the G0/G1 phase with The percentage of the G0/G1 phase is increased from 50.66 to 66.01%, in a concentration-dependent manner, induces apoptosis by increases the expression of cleaved-caspase3 and the apoptosis cell increased from 2.64% to 27.4%. |
| Animal Protocol |
Animal/Disease Models:male Balb/c nude mice (HCT116 cells)[1].
Doses: 5 mg/kg Route of Administration: I.v.; every 2 days for 16 days Experimental Results: Significantly inhibited the growth of tumors with the tumor growth reduced by 70% approximately. |
| References |
| Molecular Formula |
C52H60I2N4
|
|---|---|
| Molecular Weight |
994.87
|
| Appearance |
Typically exists as solid at room temperature
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 1.0052 mL | 5.0258 mL | 10.0516 mL | |
| 5 mM | 0.2010 mL | 1.0052 mL | 2.0103 mL | |
| 10 mM | 0.1005 mL | 0.5026 mL | 1.0052 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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