DTP3 TFA
目录号 : GC38202DTP3 is a selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor and is able to restore MKK7/JNK activation. DTP3 inhibits cancer-selective NF-κB survival pathway.
Sample solution is provided at 25 µL, 10mM.
DTP3 is a selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor and is able to restore MKK7/JNK activation. DTP3 inhibits cancer-selective NF-κB survival pathway.
DTP3 physically interacts with MKK7, both in isolation and within the complex with GADD45β, and dissociates the GADD45β/MKK7 complex via an allosteric mechanism. DTP3 selectively kills cells and induces apoptosis in MM cells with functional MKK7 and elevated GADD45β expression without toxicity to normal cells. In addition, DTP3 displays synergistic activity with bortezomib in two different MM cell lines, exhibiting a combination index of 0.21 in U266 cells and of 0.56 in KMS-12 cells. [1]
DTP3 (14.5 mg/kg/day) exhibits potent antitumor activity against MM in mouse plasmacytoma model. [1]
[1] Tornatore L, et al. Cancer Cell. 2014, 26(4), 495-508. [2] Laura Tornatore, et al. Toxicol Rep . 2019 Apr 19;6:369-379.
Cas No. | SDF | ||
分子式 | C28H36F3N7O7 | 分子量 | 639.62 |
溶解度 | Water: 100 mg/mL (156.34 mM); DMSO: 50 mg/mL (78.17 mM) | 储存条件 | -20°C, protect from light |
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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。 |
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1 mg | 5 mg | 10 mg | |
1 mM | 1.5634 mL | 7.8171 mL | 15.6343 mL |
5 mM | 0.3127 mL | 1.5634 mL | 3.1269 mL |
10 mM | 0.1563 mL | 0.7817 mL | 1.5634 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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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,
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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。
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