NSC305787 HYDROCHLORIDE
| 中文名称 | NSC305787 HYDROCHLORIDE |
|---|---|
| 中文同义词 | PKC抑制剂(NSC305787 HYDROCHLORIDE);化合物 T12263L;NSC305787盐酸盐;NSC305787盐酸盐,10 MM DMSO 溶液 |
| 英文名称 | NSC305787 (hydrochloride) |
| 英文同义词 | NSC305787 (hydrochloride);NSC-305787 HCl;NSC305787 hydrochloride,NSC-305787 hydrochloride;(2-(Adamantan-1-yl)-6,8-dichloroquinolin-4-yl)(piperidin-2-yl)methanol hydrochloride;NSC305787 hydrochloride, 10 mM in DMSO |
| CAS号 | 53868-26-1 |
| 分子式 | C25H31Cl3N2O |
| 分子量 | 481.89 |
| EINECS号 | |
| 相关类别 | 细胞生物学试剂 |
| Mol文件 | 53868-26-1.mol |
| 结构式 |  |
NSC305787 HYDROCHLORIDE 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | 二甲基亚砜：8 mg/mL（16.60 mM） |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
Kd: 5.85 μM (ezrin)
IC50: 8.3 μM (ezrin)
NSC305787 hydrochloride is an inhibitor of ezrin with a K d of 5.85 μM, and has antitumor activity. NSC305787 inhibits PKCΙ phosphorylation of Ezrin, Moesin, Radixin, MBP, with IC 50 s of 8.3, 9.4, 55, 58.9 μM, respectively. NSC305787 binds to PKCΙ with a K d value of 172.4 μM, and inhibits ezrin T567 phosphorylation primarily via its binding to ezrin and not through inhibition of PKCΙ kinase activity. NSC305787 (1, 10 μM) shows inhibitory activity against ezrin-mediated invasion of K7M2 osteosarcoma (OS) cells. Moreover, NSC305787 (10 μM) reduces cell motility phenotypes in zebrafish and blocks OS metastatic growth in lung organ culture.
NSC305787 (0.240 mg/kg/day, i.p.) suppresses ezrin-dependent osteosarcoma metastatic growth in mouse lung. NSC305787 (240 μg/kg, i.p.) dramatically inhibits pulmonary metastasis in a transgenic mouse model of osteosarcoma (Osx-Cre + p53 fl/fl pRB fl/fl ) and shows a more favorable pharmacokinetic profile compared with NSC668394 in the mouse model.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025/05/22 | HY-18931A | (Rac)-NSC305787 hydrochloride | 53868-26-1 | 1 mg | 1300元 |
| 2025/05/22 | HY-18931A | NSC305787 HYDROCHLORIDE NSC305787 hydrochloride | 53868-26-1 | 5mg | 2900元 |