PT-262
Based on 1 Customer Validation
PT-262 is a potent ROCK inhibitor with an IC50 value of around 5 μM. PT-262 induces the loss of mitochondrial membrane potential and elevates the caspase-3 activation and apoptosis. PT-262 inhibits the ERK and CDC2 phosphorylation via a p53-independent pathway. PT-262 blocks cytoskeleton function and cell migration. PT-262 has anti-cancer activity.
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- Pureza: 99.21%
- No. CAS: 86811-36-1
- Fòrmula: C14H13ClN2O2
- Peso molecular:276.72
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Almacenamiento:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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ROCK 5 μM (IC50) |
ERK |
CDK2 |
PT-262 (5-40 μM; 24 h) induces cytotoxicity and proliferation inhibition in human lung cancer cells[1].
PT-262 (2-20 μM; 4-24 h) induces caspase-3 activation, mitochondrial dysfunction and apoptosis in lung cancer cells[1].
PT-262 (10-20 μM; 24 h) induces the accumulation of G2/M phases in both the p53-wild type and p53-null lung cancer cells, and inhibits the phosphorylation of CDC2 proteins[1].
PT-262 (0-10 μM; 24 h) represses ERK phosphorylation in lung cancer cells[1].
PT-262 (2 μM; 24 h) induces the cytoskeleton alteration and cell elongation in lung carcinoma A549 cells[2].
PT-262 (2-10 μM; 6 h) significantly blocks the cell migration in a concentration-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells
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Concentration:5-40 μM
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Incubation Time:24 h
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Result:Reduced the cell viability via a concentration-dependent manner in A549 cells.
The IC50 value toward human normal lung fibroblast was >20 μM.
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Cell Line:A549 cells
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Concentration:2-20 μM
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Incubation Time:4-24 h
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Result:The apoptotic cells were increased after treatment at 10 μM for 8-24 h.
The active forms of caspase-3 (12 and 17 kD) were induced following treatment with 2-20 μM for 24 h.
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Cell Line:A549 and H1299 cells
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Concentration:10-20 μM
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Incubation Time:24 h
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Result:Significantly decreased the G1 fractions while increased the G2/M fractions in both A549 and H1299 cells with 10 μM for 24 h.
Decreased the protein levels of cyclin B1 and phospho-CDC2 at Thr14, Tyr15, and Thr161 via a concentration-dependent manner in A549 cells.
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Cell Line:A549 cells
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Concentration:0-10 μM
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Incubation Time:24 h
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Result:Significantly inhibited the phosphorylation of ERK.
Chemical Information
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No. CAS 86811-36-1
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Appearance Solid
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Peso molecular 276.72
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Fòrmula C14H13ClN2O2
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Color Brown to reddish brown
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SMILES
O=C(C(N1CCCCC1)=C2Cl)C3=C(N=CC=C3)C2=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvente y solubilidad
DMSO : 100 mg/mL (361.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Tzu-Sheng Hsu, et al. 7-Chloro-6-piperidin-1-yl-quinoline-5,8-dione (PT-262), a novel synthetic compound induces lung carcinoma cell death associated with inhibiting ERK and CDC2 phosphorylation via a p53-independent pathway. Cancer Chemother Pharmacol. 2008 Oct;62(5):799-808. [Content Brief]
[2]. Chih-Chien Tsai, et al. 7-Chloro-6-piperidin-1-yl-quinoline-5,8-dione (PT-262), a novel ROCK inhibitor blocks cytoskeleton function and cell migration. Biochem Pharmacol. 2011 Apr 1;81(7):856-65. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.6138 mL | 18.0688 mL | 36.1376 mL | 90.3440 mL |
| 5 mM | 0.7228 mL | 3.6138 mL | 7.2275 mL | 18.0688 mL | |
| 10 mM | 0.3614 mL | 1.8069 mL | 3.6138 mL | 9.0344 mL | |
| 15 mM | 0.2409 mL | 1.2046 mL | 2.4092 mL | 6.0229 mL | |
| 20 mM | 0.1807 mL | 0.9034 mL | 1.8069 mL | 4.5172 mL | |
| 25 mM | 0.1446 mL | 0.7228 mL | 1.4455 mL | 3.6138 mL | |
| 30 mM | 0.1205 mL | 0.6023 mL | 1.2046 mL | 3.0115 mL | |
| 40 mM | 0.0903 mL | 0.4517 mL | 0.9034 mL | 2.2586 mL | |
| 50 mM | 0.0723 mL | 0.3614 mL | 0.7228 mL | 1.8069 mL | |
| 60 mM | 0.0602 mL | 0.3011 mL | 0.6023 mL | 1.5057 mL | |
| 80 mM | 0.0452 mL | 0.2259 mL | 0.4517 mL | 1.1293 mL | |
| 100 mM | 0.0361 mL | 0.1807 mL | 0.3614 mL | 0.9034 mL |
PT-262 Related Classifications
HY-100035 Related Classifications
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