| CAS NO: | 827030-33-1 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Cas No. | 827030-33-1 |
| 别名 | EP128265 |
| 化学名 | 2-chloro-N-(4-methoxyphenyl)-N-methyl-4-quinazolinamine |
| Canonical SMILES | ClC(N=C1N(C2=CC=C(OC)C=C2)C)=NC3=C1C=CC=C3 |
| 分子式 | C16H14ClN3O |
| 分子量 | 299.8 |
| 溶解度 | ≤5mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | EC50: 2 nM for caspase activation MPI-0441138 is an inducer of apoptosis and growth inhibition. Apoptosis or programmed cell death is a process that organisms use to eliminate excessive cells and to control cell numbers. Caspases, a family of cysteine proteases, plays a critical role for the initiation as well as execution of apoptosis. In vitro: MPI-0441138 was identified as a highly active inducer of apoptosis and as a potent inhibitor of cell proliferation in T47D cells. MPI-0441138 also inhibited tubulin polymerization and was effective in cells overexpressing ABC transporter Pgp-1. It was found that the methyl group on the nitrogen linker was critical for the apoptosis-inducing activity [1]. In vivo: MPI-0441138 could inhibit tumor growth dose-dependently and produced >95% tumor growth inhibition with once weekly dosing at 10 mg/kg and was well tolerated. The maximum tolerated dose of MPI-0441138 was determined to be 25 mg/kg when dosed once weekly, resulting in a good therapeutic index of 2.5. In addition, MPI-0441138 at a dose of 2.5 mg/kg could produce 90% tumor growth inhibition in the MX-1 model when dosed once every day for 5 days for 2 weeks. Furthermore, in nude mice, MPI-0441138 significantly inhibited the growth of human PC-3 prostate cancer xenografts [1]. Clinical trial: Up to now, MPI-0441138 is still in the preclinical development stage. Reference: |
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