| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
PKM2-IN-12 (Compound 10j) (24 h) showed significantly different sensitivities in COLO-205, CAL-27 and MCF-7 cells, with IC50 values of 4.21, 13.3 and 22.34 μM, respectively [1]. PKM2-IN-12 (4.21 μM, 48 h) mainly killed COLO-205 cells by inducing late apoptosis and arrested the cells in the G2 phase [1]. PKM2-IN-12 (4.21 μM) significantly inhibited the migration ability of COLO-205 cells [1]. PKM2-IN-12 (4.21 μM, 0-48 h) significantly reduced the levels of lactate, pyruvate and reactive oxygen species (ROS) in COLO-205 cells [1]. PKM2-IN-12 (4.21 μM, 48 h) increased the expression of PKM2 monomers and tetramers in COLO-205 cells, but had no effect on PKM1[2].
|
|---|---|
| ln Vivo |
PKM2-IN-12 (Compound 10j) (50-100 mg/kg, appendix, every three days for 72 days) effectively reversed tumor growth in an inflammatory colorectal cancer (CAC) model and reversed torsion-induced microbial imbalance [1].
|
| Animal Protocol |
Animal/Disease Models: AOM/DSS induced colitis-associated colorectal cancer (CAC) model established in BALB/c mice[1]
Doses: 50, 75 and 100 mg/kg Route of Administration: Oral administration (p.o,), once every three days for 72 days Experimental Results: Significantly inhibited tumor formation and reduce tumor burden. Increased the length of the colon, and maintain the stable weight of the mice. Significantly restored the alpha diversity of the intestinal microbiota in mice. Reduced the pathological scores of the colon tissue, including inflammatory cell infiltration, epithelial damage and abnormal glandular structure. |
| References |
| Molecular Formula |
C23H14CL2N4OS
|
|---|---|
| Molecular Weight |
465.35
|
| Appearance |
Typically exists as solids 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 | 2.1489 mL | 10.7446 mL | 21.4892 mL | |
| 5 mM | 0.4298 mL | 2.1489 mL | 4.2978 mL | |
| 10 mM | 0.2149 mL | 1.0745 mL | 2.1489 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
