| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
MCC1019 can efficiently and selectively inhibit PLK1 PBD, with an IC50 value of 16.4 μM in cell-free biochemical experiments [1]. MCC1019 can inactivate the AKT signaling pathway, inhibit cell replication, and induce mitotic catastrophe in lung adenocarcinoma A549 cells [1]. MCC1019 can bind to PLK1 (Kd = 12.77 μmol/L) and PLK1 PBD (Kd = 18.9 μmol/L) [2]. MCC1019 (10-40 μmol/L; 24 hours) can induce G2/M phase cell cycle arrest in human lung adenocarcinoma A549 cells in a concentration-dependent manner [2]. MCC1019 (40 μmol/L; 48 hours) can induce autophagy in lung adenocarcinoma cell line A549 [2].
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| ln Vivo |
MCC1019 (20-40 mg/kg; intraperitoneal injection; once daily; for 16 days) inhibited lung tumor growth by 51.1% and 68.1% respectively in a homologous mouse lung cancer model, while reducing lung metastasis burden and exhibiting extremely low systemic toxicity [2]. MCC1019 (40 mg/kg; intraperitoneal injection; once daily; for 14 days) inhibited prostate tumor growth by 61.5% in a homologous mouse prostate cancer model without causing significant changes in body weight [2]. MCC1019 (100-200 mg/kg; oral administration; once daily; for 7 days) achieved 100% survival in healthy C57BL/6 mice without causing significant weight loss [2].
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| Cell Assay |
Cytotoxicity assay [2] Cell Types: Human cancer cell lines (A549, K562, MCF-7, HCT116 p53+/+, HepG2, U87MG, CCRF-CEM, CEM/ADR5000) Concentrations tested: 0.001-100 μmol/L
Incubation Duration: 72 hours Experimental Results: All tested cell lines showed cytotoxicity, with IC50 values of 23.7 ± 3.7 μmol/L (A549), 2.2 ± 0.09 μmol/L (K562), 25.4 ± 4.08 μmol/L (MCF-7), and 18.7 ± 2.8 μmol/L (HCT116 p53+/+). p53+/+), 21.3 ± 3.6 μmol/L (HepG2), 22.7 ± 6.06 μmol/L (U87MG), 1.6 ± 0.24 μmol/L (CCRF-CEM), and 1.3 ± 0.4 μmol/L (CEM/ADR5000). |
| Animal Protocol |
Animal/Disease Models:C57BL/6 mice (male and female, 8 weeks old, weighing 25 ± 5 g, homologous model established by subcutaneous injection of LLC-1 lung cancer cells)[2]
Doses: 20 mg/kg; 40 mg/kg Route of Administration: Intraperitoneal injection; once daily; for 16 days Experimental Results: Induced tumor growth inhibition of 51.1% and reduced the mean lung metastasis burden area to 0.1% (compared to 4.1% in the control group). Induced tumor growth inhibition of 68.1% and reduced the mean lung metastasis burden area to 2.1%. No significant changes in body weight or the weight of the heart, liver, lungs or kidneys were observed (only a slight change in spleen weight was observed). Downregulated BUBR1 expression in LLC-1 tumors. |
| References |
|
| Molecular Formula |
C12H11BRO3
|
|---|---|
| Molecular Weight |
283.12
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| CAS # |
29115-34-2
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C(OCC)C=1OC=2C=CC=CC2C1CBr
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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 | 3.5321 mL | 17.6604 mL | 35.3207 mL | |
| 5 mM | 0.7064 mL | 3.5321 mL | 7.0641 mL | |
| 10 mM | 0.3532 mL | 1.7660 mL | 3.5321 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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