PhiKan 083 HCl

产品说明书

Print
Chemical Structure| 1050480-30-2 同义名 : PhiKan 083 hydrochloride
CAS号 : 1050480-30-2
货号 : A1176637
分子式 : C16H19ClN2
纯度 : 99%+
分子量 : 274.788
MDL号 : -
存储条件：

Pure form Inert atmosphere,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(218.35 mM)，配合低频超声，并水浴加热至45℃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

H2O: 2 mg/mL(7.28 mM)
动物实验配方：
生物活性
描述 PhiKan 083 HCl is a carbazole derivative that binds to surface cavities and stabilises the p53 Y220C mutant with a Kd value of 167 μM[1].PhiKan 083 HCl has a Kd value of 150 μM in Ln229 cells. At a concentration of 125 μM for 48 hours, PhiKan 083 HCl reduces the cell viability of the engineered variants of Ln229 cells. PhiKan 083 (100 μM) in combination with NSC 123127 (1 μM) enhances the pro-apoptotic activity of all variants of Ln229 cells ( p53wt, p53Y220C, p53G245S, p53R282W). After 48 hours of action, it resulted in a 70 ± 5% reduction in viability of Ln229 variant cells[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.64mL

0.73mL

0.36mL

18.20mL

3.64mL

1.82mL

36.39mL

7.28mL

3.64mL
参考文献

[1]Boeckler FM, et al. Targeted rescue of a destabilized mutant of p53 by an in silico screened drug. Proc Natl Acad Sci U S A. 2008 Jul 29;105(30):10360-5.

[2]Paulmurugan R, et al. A protein folding molecular imaging biosensor monitors the effects of drugs that restore mutant p53 structure and its downstream function in glioblastoma cells. Oncotarget. 2018 Apr 20;9(30):21495-21511.