| ln Vitro |
The antitumor drug-214 (compound 3f) showed cytotoxic activity against HCT-116 cells (IC50 = 3.56 μM), MCF-7 cells (IC50 = 4.08 μM), A549 cells (IC50 = 12.70 μM), HeLa cells (IC50 = 8.37 μM), HT-29 cells (IC50 = 6.18 μM) and MD-MBA-231 cells (IC50 = 10.62 μM), but had low cytotoxic activity against non-cancer cells MCF-10AMCF-10A (IC50 = 9.81 μM) [1]. The antitumor drug-214 (1.78-7.12 μM; 24 h) can cause HCT-116 cells to accumulate in a dose-dependent manner in the sub-G1 phase, indicating that it can induce apoptosis [1]. Antitumor drug-214 (3.56 μM, 7.12 μM; 24 h) can induce apoptosis in HCT-116 cells, as confirmed by Annexin V-FITC/PI double staining. Its apoptosis rate is comparable to that of astrococcus, but its apoptosis effect on MCF-10A cells is weaker [1]. Antitumor drug-214 (3.56 μM, 7.12 μM; 24 h) can induce apoptosis in HCT-116 cells, as confirmed by AO-EB double staining. The proportion of orange fluorescent apoptotic cells increases in a dose-dependent manner [1]. Antitumor drug-214 (3.56 μM, 7.12 μM; 24 h) can increase the production of mitochondrial superoxide in HCT-116 cells, as confirmed by MitoSOX Red staining [1]. The antitumor drug-214 (7.12 μM; 24 hours) can induce depolarization of the mitochondrial transmembrane potential in HCT-116 cells, which was confirmed by JC-1 staining results [1]. The antitumor drug-214 (7.12 μM; 4-12 hours) can promote the cleavage of PARP1, caspase 3, caspase 7 and caspase 9 in HCT-116 cells. Western blot analysis showed that the cleaved proteins accumulated significantly at 12 hours [1].
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| Cell Assay |
Cell cycle analysis [1]
Cell Types: HCT-116 cells Tested Concentrations: 1.78 μM, 3.56 μM, 7.12 μM Incubation Duration: 24 hours Experimental Results: Induced significant dose-dependent accumulation of cells in the sub-G1 phase, but had no significant effect on the distribution of cells in the G0/G1, S, and G2/M phases. Apoptosis analysis [1] Cell Types: HCT-116 cells Tested Concentrations: 3.56 μM, 7.12 μM Incubation Duration: 24 hours Experimental Experimental Results: Antitumor drug 214 induced apoptosis in a dose-dependent manner, and the percentage of apoptosis induced by it was comparable to that induced by the positive control astrosporin (STS). Apoptosis analysis [1] Cell Types: MCF-10A cells Tested Concentrations: 9.81 μM, 19.62 μM Incubation Duration: 24 hours Experimental Experimental Results: Antitumor drug 214 induced apoptosis in a dose-dependent manner. The percentage of apoptosis induced by it was only 54% of that induced by STS, indicating that its apoptosis-inducing ability in normal cells was lower than that in cancer cells.
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| References |
| CAS # |
1911631-77-0
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| 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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