| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
PLK1 PBD
|
|---|---|
| ln Vitro |
PLK1-IN-10 (0-6 μM; 48 h) induces cell cycle arrest in G2/M phase of A549 and A549/DDP, inhibiting cell proliferation[1]. PLK1-IN-10 (20 μM) can stabilize PLK1 protein in A549/DDP at different temperature ranges[1]. PLK1-IN-10 (5 μM; 24 h) reacts with GSH to produce a dose- and time-dependent fluorescence response, with higher fluorescence intensity in A549/DDP cells[1]. PLK1-IN-10 (0-9 μM; 48 h) increases intracellular ROS level in A549/DDP[1]. PLK1-IN-10 (10 μM; 48 h) inhibits the interaction between PLK1 and PRC1, resulting in multinuclear phenomenon[1]. The anticancer activity of PLK1-IN-10 against NCI-H1975 cells is IC50=7.83 μM[1].
|
| ln Vivo |
PLK1-IN-10 (30, 50 mg/kg; ip; once every two days for 32 days) significantly inhibited tumor growth in A549/DDP-resistant xenograft mice, and the 50 mg/kg group even caused tumor regression [1 ]. PLK1-IN-10 (30 mg/kg; po; once every two days for 20 days) effectively inhibits tumor growth in NCI–H1975-resistant xenograft mice [1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: A549, A549/DDP Concentration: 0, 1.5, 3, 6 μM Incubation Duration: 48 h Experimental Results: Downregulated the expression of PLK1, CDK1, Cyclin B1, as well as significantly downregulated the expression of the CDK1-Cyclin B1 complex and Cdc25 protein. Cell Cycle Analysis[1] Cell Types: A549, A549/DDP Concentration: 0, 1.5, 3, 6 μM Incubation Duration: 48 h Experimental Results: Significantly increased the number of A549 and A549/DDP cells in the G2/M phase, inducing mitotic catastrophe. |
| Animal Protocol |
Animal/Disease Models:A549/DDP drug-resistant xenograft mice[1]
Doses: 30, 50 mg/kg Route of Administration: i.p.; once every two days for 32 days Experimental Results: TGI reached 42% for the 30 mg/kg group and 62% for the 50 mg/kg group. Extended the median survival time from 38 days in the control group to 53 days in the 30 mg/kg group and 62 days in the 50 mg/kg group. Had no significant impact on the body weight and major organs of the mice, except for a slight difference in heart index observed in the 30 mg/kg group. Significantly reduced the number of Ki-67 positive cells in the tumor tissue. Showed no significant differences in H&E staining of major organs, further confirming its good biosafety. |
| References |
| Molecular Formula |
C23H22FN3O4S
|
|---|---|
| Molecular Weight |
455.50
|
| CAS # |
2991469-21-5
|
| Appearance |
Typically exists as solid 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 | 2.1954 mL | 10.9769 mL | 21.9539 mL | |
| 5 mM | 0.4391 mL | 2.1954 mL | 4.3908 mL | |
| 10 mM | 0.2195 mL | 1.0977 mL | 2.1954 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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