Pyridoclax
Pyridoclax 是一种潜在的 Mcl-1 抑制剂。
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包装价格促销价数量
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5mg￥875.00700.00- +
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10mg￥1487.001190.00- +
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50mg￥5150.004120.00- +
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100mg￥5475.004380.00- +
- 货号: ajcx11176
- CAS: 1651890-44-6
- 别名: MR-29072
- 分子式: C29H22N4
- 分子量: 426.51
- 纯度: ＞98%
- 溶解度: Soluble in DMSO
- 储存: Store at -20°C
- 库存: 现货
Background
Pyridoclax is a potential Mcl-1 inhibitor.
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].
参考文献:
[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.
[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.
Protocol
Kinase experiment: | 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]. |
参考文献: [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. | |
