| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
PDK1-IN-5 (compound D16) (48 h) showed selectivity and excellent antiproliferative activity against A549 (lung adenocarcinoma), PC9 (lung adenocarcinoma), H1975 (human non-small cell lung adenocarcinoma), HGC-27 (gastric cancer) and HCT-116 (colorectal cancer) cells, with IC50 values of 0.86, 5.99, 4.92, 2.48 and 1.15 μM, respectively [1]. PDK1-IN-5 showed strong PDK1 inhibitory activity with an inhibition rate of 53.20% [1]. PDK1-IN-5 (0-12 μM, 0.5 h) reduced the phosphorylation level of PDH in A549 and PC9 cells by inhibiting PDK1 activity, thereby activating PDH [1]. PDK1-IN-5 (0.4-1.6 μM, 14 days) inhibited the proliferation of A549 and PC9 cells in a concentration-dependent manner [1]. PDK1-IN-5 (0.4-1.6 μM and 3-12 μM, 24 hours) inhibited the migration of A549 and PC9 cells in a dose-dependent manner [1]. PDK1-IN-5 (0.2-3.2 μM and 1.5-24 μM, 48 hours) increased mitochondrial ROS levels and induced concentration-dependent apoptosis [1]. PDK1-IN-5 (0.2-3.2 μM and 1.5-24 μM, 24 and 48 hours) reversed the Warburg effect by potently inhibiting PDK1, thereby effectively altering tumor cell metabolism and shifting the energy balance from glycolysis to oxidative phosphorylation, highlighting its therapeutic potential [1].
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|---|---|
| ln Vivo |
PDK1-IN-5 (compound D16) (5-20 mg/kg, intraperitoneal injection, once every 2 days for 1 day) exerted its tumor-inducing effect by inhibiting tumor swelling in A549 and PC9 xenograft models [1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: A549 and PC9 cells Tested Concentrations: 0, 0.4, 0.8 and 1.6 μM (A549); 0, 3, 6, 12 μM (PC9) Incubation Duration: 0.5 h Experimental Results: Decreased the expression of phosphorylated protein pPDH (serine 293) in a concentration-dependent manner. Reduced phosphorylation level and raised PDHA1 expression. Cell Proliferation Assay[1] Cell Types: A549 and PC9 cells Tested Concentrations: 0, 0.4, 0.8 and 1.6 μM (A549); 0, 3, 6, 12 μM (PC9) Incubation Duration: 14 days Experimental Results: Achieved 98 % inhibition of colony formation at 14 day in high concentration treatment (1.6 μM). Cell Migration Assay [1] Cell Types: A549 and PC9 cells Tested Concentrations: 0, 0.4, 0.8 and 1.6 μM (A549); 0, 3, 6, 12 μM (PC9) Incubation Duration: 24 h Experimental Results: Reached 80.5 % inhibition at the highest concentration. Cell Cytotoxicity Assay[1] Cell Types: A549 and PC9 cells Tested Concentrations: 0.2, 0.8 and 3.2 μM (A549); 1.5, 6, 24 μM (PC9) Incubation Duration: 48 h Experimental Results: Induced PC9 cells apoptotic rate at 1.5, 6, and 24 μM with 7.0%, 12.5%, and 17.7%, respectively. Induced A549 cells apoptotic rate at 0.2, 0.8, and 3.2 μM with 16.1%, 26.6%, and 30.7%, respectively. |
| Animal Protocol |
Animal/Disease Models: Male BALB/c-nu nude mice (4 weeks old) were implanted with A549 and PC9 cells[1].
Doses: 5, 10, and 20 mg/kg Route of Administration: i.p., every 2 days for 14 days Experimental Results: Revealed no pathological abnormalities in Hematoxylin-Eosin (H&E) in major organs (heart, liver, spleen, lung, kidney) from the 20 mg/kg. Maintained stable body weights in animals throughout the experimental period. Downregulated PDK1 expression and reduced the number of Ki-67-positive cells in treated tumors. |
| References |
| Molecular Formula |
C16H12CL2F3NO3
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|---|---|
| Molecular Weight |
394.17
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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)
|
| 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 | 2.5370 mL | 12.6849 mL | 25.3698 mL | |
| 5 mM | 0.5074 mL | 2.5370 mL | 5.0740 mL | |
| 10 mM | 0.2537 mL | 1.2685 mL | 2.5370 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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