| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Apoptosis inducer 43 (compound 5f) (10 μM) showed anticancer activity, with an average inhibition rate of over 80% against NCI 60 cells (leukemia, non-small cell lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer and breast cancer) and an average GI50 of less than 5 μM[1]. Apoptosis inducer 43 (1.79-10 μM, 24 hours) can induce cell cycle arrest, mainly in the SubG0/G1 phase, and induce apoptosis in HCT-116 cells[1].
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|---|---|
| ln Vivo |
Apoptosis inducer 43 (compound 5f) (10 mg/kg, intraperitoneal injection, three times a week for 14 days) showed antitumor activity in a mouse model of solid Ehrlich cancer (SEC) [1].
|
| Cell Assay |
Cell cycle analysis [1]
Cell Types: HCT-116 cells Tested Concentrations: 10 μM Incubation Duration: 24 hours Experimental Results: The cell cycle distribution was induced to change, resulting in cell cycle arrest in the sub-G0-G1 phase. The percentage of cells in the G0/G1 phase increased from 7% (control group) to 44%. This led to a decrease in the percentage of cells in the other phases (G0-G1 phase, S phase and G2/M phase). Apoptosis analysis [1] Cell Types: HCT-116 cells Tested Concentrations: 1.79 μM Incubation Duration: 24 hours Experimental Results: Percentage of live cells decreased, percentage of necrotic cells increased. Levels of caspase-3, p53 and Bax proteins increased, while level of Bcl-2 protein decreased. |
| Animal Protocol |
Animal/Disease Models:SEC (0.2 mL/mouse) female Swiss albino mice (18-22g) model [1]
Doses: 10 mg/kg Route of Administration: Intraperitoneal injection, three times a week for 14 days Experimental Results: Anti-tumor effect was observed, with tumor volume reduced by 72.5% and tumor weight reduced by 76%. Tumor cells were distributed in small foci, with obvious mitotic figures and large areas of necrosis surrounding them. Mitotic cell count and VEGF expression were both reduced. |
| References |
| Molecular Formula |
C32H27F3N2O4
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|---|---|
| Molecular Weight |
560.56
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(NC1=CC=CC(C(/C=C/C2=CC=C(C3=CC=CC=C3)C=C2)=O)=C1)C([NH3+])CC4=CC=CC=C4.FC(F)(F)C([O-])=O
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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 | 1.7839 mL | 8.9197 mL | 17.8393 mL | |
| 5 mM | 0.3568 mL | 1.7839 mL | 3.5679 mL | |
| 10 mM | 0.1784 mL | 0.8920 mL | 1.7839 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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