Size | Price | |
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500mg | ||
1g | ||
Other Sizes |
Targets |
PKM2, PDK-1[1]
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ln Vitro |
PKM2/PDK1-IN-1(compound E5)(0.5–4 μM; 24 h) and gefitinib (HY–50895) exhibit complementary anti-tumor effects[1]. Death receptor pathways and mitochondrial apoptotic proteins are regulated by PKM2/PDK1-IN-1 (0.5 μM; 24 h) [1]. Lung cancer cells exhibit intracellular ROS generation and mitochondrial transmembrane potential (ΔΨm) dissipation when exposed to PKM2/PDK1-IN-1 (0.5 μM, 1 μM; 24 h) [1]. Inhibiting PDK1 and increasing downstream PDH activity in H1975 cells, PKM2/PDK1-IN-1 (1 μM, 2 μM; 24 hours) [1]. PKM2/PDK1-IN-1 enhances the generation of ATP in H1975 cells while inhibiting the intracellular concentration of NADPH [1]. .
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ln Vivo |
PKM2/PDK1-IN-1 (compound E5) (2.4 mg/kg, 4.8 mg/kg; six times in two days, totaling 11 days) had no harmful and side effects while inhibiting the formation of H1975 xenograft tumors in nude mice in vivo [1].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: H1975 cells Tested Concentrations: 0.5 μM, 1 μM, 2 μM, 4 μM24 h; with 2.5-20 μM Gefitinib Incubation Duration: 24 h Experimental Results: Synergistically induced cell apoptosis. Western Blot Analysis[1] Cell Types: H1975 cells Tested Concentrations: 0.5 μM Incubation Duration: 24 h; with 10 μM Gefitinib Experimental Results: Increased the protein levels of Cleaved Caspase-9, -3, and Cytochrome c. Deceased the protein levels of p-AKT, p-EGFR, Bcl-2. |
Animal Protocol |
Animal/Disease Models: Nude mice with H1975 xenograft tumor (6weeks old)[1]
Doses: 4.8 mg/kg; dispersed in 20% DMSO Route of Administration: IP; every two days for a total of 6 times, for 11 days Experimental Results: Inhibited tumor growth. Animal/Disease Models: For acute toxicity in ICR mice (8weeks old)[1] Doses: 2.4, 4.8, 9.6, 19.2, 38.4 mg/kg; dissolved in 20% DMSO Route of Administration: IP; singel dose; observed for 14 days Experimental Results: demonstrated little side effect in mice. |
References |
Molecular Formula |
C36H43NO7S3
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Molecular Weight |
697.92
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Appearance |
Typically exists as solid 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.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.4328 mL | 7.1641 mL | 14.3283 mL | |
5 mM | 0.2866 mL | 1.4328 mL | 2.8657 mL | |
10 mM | 0.1433 mL | 0.7164 mL | 1.4328 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.