| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
In human lung cancer cells, PT-262 (5–40 μM; 24 hours) causes cytotoxicity and growth inhibition [1]. Lung cancer cells are exposed to PT-262 (2–20 μM; 4–24 hours) which causes caspase-3 activation, mitochondrial malfunction, and apoptosis [1]. PT-262 (10–20 μM; 24 hours) suppresses the phosphorylation of CDC2 protein and causes p53 to accumulate in the G2/M phase in lung cancer cells with and without p53 [1]. In lung cancer cells, PT-262 (0-10 μM; 24 hours) suppresses ERK phosphorylation [1]. In lung cancer A549 cells, PT-262 (2 μM; 24 h) causes cytoskeletal alterations and cell elongation [2]. Cell migration is strongly inhibited by PT-262 (2-10 μM; 6 hours) in a concentration-dependent manner [2].
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|---|---|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: A549 Cell Tested Concentrations: 5-40 μM Incubation Duration: 24 hrs (hours) Experimental Results: Cell viability diminished in A549 cells in a concentration-dependent manner. The IC50 value for human normal lung fibroblasts is >20 μM. Cell apoptosis analysis [1] Cell Types: A549 cells Tested Concentrations: 2-20 μM Incubation Duration: 4-24 h Experimental Results: After 8-24 h treatment with 10 μM, the number of apoptotic cells increased. Active forms of caspase-3 (12 and 17 kD) were induced after 24 h of treatment with 2-20 μM. Cell cycle analysis [1] Cell Types: A549 and H1299 Cell Tested Concentrations: 10-20 μM Incubation Duration: 24 hrs (hours) Experimental Results: After 10 μM for 24 hrs (hours), the G1 fraction in A549 and H1299 cells Dramatically diminished, and the G2/M fraction increased. In A549 cells, protein levels of cyclin B1 and phosphorylated CDC2 were diminished at Thr14, Tyr15, and Thr161 in a concentration-dependent manner. Western Blot Analysis [1] Cell Types: A549 cells Tested Concentrations: 0-10 μM Incubation Duration: 24 h Experimental Results: S |
| References |
|
| Molecular Formula |
C14H13CLN2O2
|
|---|---|
| Molecular Weight |
276.72
|
| Exact Mass |
276.066
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| CAS # |
86811-36-1
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| PubChem CID |
12424014
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| Appearance |
Brown to reddish brown solid powder
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| LogP |
2.7
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
19
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| Complexity |
441
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C1C2C=CC=NC=2C(=O)C(Cl)=C1N1CCCCC1
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| InChi Key |
XBHXHCMFAUSIKK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C14H13ClN2O2/c15-10-12(17-7-2-1-3-8-17)13(18)9-5-4-6-16-11(9)14(10)19/h4-6H,1-3,7-8H2
|
| Chemical Name |
7-chloro-6-piperidin-1-ylquinoline-5,8-dione
|
| Synonyms |
PT-262 PT262 PT 262
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
DMSO : ~100 mg/mL (~361.38 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.03 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6138 mL | 18.0688 mL | 36.1376 mL | |
| 5 mM | 0.7228 mL | 3.6138 mL | 7.2275 mL | |
| 10 mM | 0.3614 mL | 1.8069 mL | 3.6138 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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