PHIKAN 083
| 中文名称 | PHIKAN 083 |
|---|---|
| 中文同义词 | 化合物PHIKAN 083;1-(9-乙基-9H-咔唑-3-基)-N-甲基甲胺 |
| 英文名称 | PhiKan-083 Hydrochloride |
| 英文同义词 | PhiKan-083 Hydrochloride;PhiKan 083;[(9-Ethyl-9H-carbazol-3-yl)methyl](methyl)amine;9-Ethyl-N-methyl-carbazole-3-methanamine;PK083;9-Ethyl-N-methyl-9H-carbazole-3-methanamine hydrochloride;9H-Carbazole-3-methanamine, 9-ethyl-N-methyl-;PhiKan 083,PhiKan-083,Inhibitor,MDM-2/p53,PhiKan083,inhibit |
| CAS号 | 880813-36-5 |
| 分子式 | C16H18N2 |
| 分子量 | 238.33 |
| EINECS号 | |
| 相关类别 | Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals |
| Mol文件 | 880813-36-5.mol |
| 结构式 |  |
PHIKAN 083 性质
| 沸点 | 401.0±27.0 °C(Predicted) |
|---|---|
| 密度 | 1.09±0.1 g/cm3(Predicted) |
| 储存条件 | Store at 4°C |
| 溶解度 | <13.74mg/ml，在水中； <27.48mg/ml，溶于 DMSO |
| 形态 | 固体 |
| 酸度系数(pKa) | 9.71±0.10(Predicted) |
| 颜色 | 白色 |
Kd: 167 μM (p53-Y220C), 150 μM (p53 Y220C , in Ln229 cells)
PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes
Y220C
(a
p53
mutant), with a
K
d
of 167 μM, shows a relative binding affinity (K
d
) of 150 μM for p53
Y220C
in Ln229 cells.
PhiKan 083 slows down its thermal denaturation rate.
PhiKan 083 (125 μM, 48 hours) reduces the cell viability of engineered variants of Ln229 cells.
PhiKan 083 (100 μM) in conbination with NSC 123127 (1 μM) enhances the pro-apoptotic activity in all variants of Ln229 cells (p53
wt
, p53
Y220C
, p53
G245S
, p53
R282W
).
Cell Viability Assay
| Cell Line: | Ln229, Ln229-p53-wt, Ln229-p53-Y220C, Ln229-p53-G245S, Ln229-p53-R282W cells |
| Concentration: | 125 μM |
| Incubation Time: | 48 hours |
| Result: | Caused ∼70 ± 5% reduction in cell viability of variants of Ln229 cells. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-108637A | PHIKAN 083 PhiKan 083 hydrochloride | 880813-36-5 | 5mg | 1100元 |
| 2024/08/19 | HY-108637A | PhiKan 083 hydrochloride | 10 mg | 1760元 |