產(chǎn)品目錄

規(guī)格	1mg 5mg 10mg 25mg
CAS	827030-33-1
別名	EP128265
化學(xué)名	2-chloro-N-(4-methoxyphenyl)-N-methyl-4-quinazolinamine
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
儲存條件	Store at -20°C
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

產(chǎn)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.

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請穿好實驗服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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