CB-103

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Chemical Structure| 218457-67-1 同义名 : -
CAS号 : 218457-67-1
货号 : A176056
分子式 : C15H18N2O
纯度 : 98%
分子量 : 242.316
MDL号 : MFCD00052647
存储条件:

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(433.32 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Limantrafin (CB-103) is a pioneering, orally bioavailable inhibitor of protein-protein interaction (PPI) targeting the NOTCH transcriptional activation complex. Limantrafin exhibits antitumor efficacy[1][2][3][4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.13mL

0.83mL

0.41mL

20.63mL

4.13mL

2.06mL

41.27mL

8.25mL

4.13mL

参考文献

[1]Freddy Radtke, et al. Inhibitors of notch signalling pathway and use thereof in treatment of cancers. US9296682B2.

[2]R.Lehal, et al. Development of a novel first-in-class oral inhibitor of the NOTCH pathway.

[3]Rajwinder Lehal, et al. Non clinical pharmacology, pharmacokinetics and safety profiling of CB-103: A novel first-in-class small molecule inhibitor of the NOTCH pathway.

[4]Jose Manuel Perez Garcia, et al. First-in-human phase 1-2A study of CB-103, an oral Protein-Protein Interaction Inhibitor targeting pan-NOTCH signalling in advanced solid tumors and blood malignancies.