| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
PLK1-IN-16 (compound B7) inhibited the proliferation of MDA-MB-231, MDA-MB-361 and MV-4-11 cells, with IC50 values of 72.5 nM, 316 nM and 32.1 nM, respectively [1]. PLK1-IN-16 (12.5-200 nM; 72 h) arrested MV-4-11 cells in the G2 phase in a dose-dependent manner [1]. PLK1-IN-16 (5.0-80.0 nM; 72 h) induced apoptosis in MV-4-11 cells in a dose-dependent manner [1]. PLK1-IN-16 (2 h) was stable under simulated gastric acid conditions, with a residual rate of 98.4% after 2 h [1]. PLK1-IN-16 showed weak inhibitory effects on CYP1A2, CYP2C9, CYP2C19 and CYP2D6, but strong inhibitory effects on CYP3A4 (IC50 approximately 1 μM) [1]. PLK1-IN-16 exhibited high plasma protein binding rates in human (99.6%), rat (99.7%) and mouse (99.4%) plasma [1].
|
|---|---|
| ln Vivo |
PLK1-IN-16 (compound B7) (20 mg/kg; orally; once) showed high safety in mice, with normal growth and development, and no obvious physiological abnormalities or lesions were observed in the heart, liver, spleen, lungs and kidneys [1].
|
| Cell Assay |
Cell cycle analysis [1]
Cell Types: MV-4-11 Tested Concentrations: 12.5 nM, 25.0 nM, 50.0 nM, 100 nM and 200 nM Incubation Duration: 72 hours Experimental Results: G2 phase arrest was induced in a dose-dependent manner, and 4N DNA aggregation was observed starting from 100 nM. Apoptosis analysis [1] Cell Types: MV-4-11 Tested Concentrations: 5.0 nM, 10.0 nM, 20.0 nM, 40.0 nM and 80.0 nM Incubation Duration: 72 hours Experimental Results: Apoptosis rate increased in a concentration-dependent manner, ranging from 10.98% to 34.09%. |
| References |
| Molecular Formula |
C26H34N6O4S
|
|---|---|
| Molecular Weight |
526.65
|
| CAS # |
3068378-51-5
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=S(N1C2=CC(OC)=C(NC3=NC=C4C(N(C5CCCC5)[C@H](CC)C(N4C)=O)=N3)C=C2CC1)(C6CC6)=O
|
| 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 | 1.8988 mL | 9.4940 mL | 18.9879 mL | |
| 5 mM | 0.3798 mL | 1.8988 mL | 3.7976 mL | |
| 10 mM | 0.1899 mL | 0.9494 mL | 1.8988 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
