MPI-0441138
(Synonyms: EP128265) 目录号 : GC14050
A potent inducer of apoptosis and growth inhibition
Cas No.:827030-33-1
Sample solution is provided at 25 µL, 10mM.
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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:
[1] N. Sirisoma, S. Kasibhatla, A. Pervin, et al. Discovery of 2-chloro-N-(4-methoxyphenyl)-N-methylquinazolin-4-amine (EP128265, MPI-0441138) as a potent inducer of apoptosis with high in vivo activity. Journal of Medicinal Chemistry 51, 4771-4779 (2008).
| Cas No. | 827030-33-1 | SDF | |
| 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°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3356 mL | 16.6778 mL | 33.3556 mL |
| 5 mM | 667.1 μL | 3.3356 mL | 6.6711 mL |
| 10 mM | 333.6 μL | 1.6678 mL | 3.3356 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet