Pyridoclax
Based on 1 publication(s) in Google Scholar
Pyridoclax is a potential Mcl-1 inhibitor.
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- Pureté: 99.95%
- CAS No.: 1651890-44-6
- Formule: C29H22N4
- Masse moléculaire:426.51
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Pyridoclax
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Activité biologique
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Mcl-1 |
Pyridoclax directly binds to Mcl-1. Without cytotoxic activity when administered as a single agent, Pyridoclax induces apoptosis in combination with Bcl-xL-targeting siRNA or with ABT-737 in ovarian, lung, and mesothelioma cancer cells[1]. Pyridoclax directly binds to Mcl-1, and hence sensitizes ovarian carcinoma cells to Bcl-xL-targeting strategies. Pyridoclax induces apoptosis in ovarian, and also in lung, and mesothelioma cancer cells when it is administrated in combination with Bcl-xL-targeting siRNA or Bcl-xL targeting molecules such as ABT-737 or its orally available derivative ABT-263[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1651890-44-6
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Appearance Solid
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Masse moléculaire 426.51
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Formule C29H22N4
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Color White to off-white
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SMILES
CC1=CC(C2=NC=C(C3=CC=CN=C3)C=C2/C=C/C4=CC=CC=C4)=CN=C1C5=CC=CN=C5
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Synonyms
MR-29072
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Methods Mol Biol
2018:1711:351-398. PMID: 29344898
Solvant et solubilité
DMSO : 20 mg/mL (46.89 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocole
For donor saturating assays, Hela cells are seeded on 12-well plates and transfected with 200 ng/well of plasmid pRluc-BimL coding for BRET donor and an increasing quantity of BRET acceptor plasmids peYFP-Mcl-1 (or with pCMV-Mcl-1 as a control). Twenty-four hours after transfection, cells are trypsinized, reseeded into white flat bottom 96-well plates, and incubated for another day before measurements. A single donor/acceptor ratio (200/800) is used to carry out the drug treatment assay. After reseeding, cells are then subject to a 16 h Pyridoclax treatment. Light emission at 485 and 530 nm is measured consecutively using the Mithras fluorescence-luminescence detector LB 940 after adding the luciferase substrate, coelenterazine H, at a final concentration of 5 μM. BRET ratios are calculated[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (277 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)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Gloaguen C, et al. First evidence that oligopyridines, α-helix foldamers, inhibit Mcl-1 and sensitize ovarian carcinoma cells to Bcl-xL-targeting strategies. J Med Chem. 2015 Feb 26;58(4):1644-68. [Content Brief]
[2]. Groo AC, et al. Comparison of 2 strategies to enhance Pyridoclax solubility: Nanoemulsion delivery system versus salt synthesis. Eur J Pharm Sci. 2017 Jan 15;97:218-226. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3446 mL | 11.7231 mL | 23.4461 mL | 58.6153 mL |
| 5 mM | 0.4689 mL | 2.3446 mL | 4.6892 mL | 11.7231 mL | |
| 10 mM | 0.2345 mL | 1.1723 mL | 2.3446 mL | 5.8615 mL | |
| 15 mM | 0.1563 mL | 0.7815 mL | 1.5631 mL | 3.9077 mL | |
| 20 mM | 0.1172 mL | 0.5862 mL | 1.1723 mL | 2.9308 mL | |
| 25 mM | 0.0938 mL | 0.4689 mL | 0.9378 mL | 2.3446 mL | |
| 30 mM | 0.0782 mL | 0.3908 mL | 0.7815 mL | 1.9538 mL | |
| 40 mM | 0.0586 mL | 0.2931 mL | 0.5862 mL | 1.4654 mL |
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