目錄:MedChemExpress LLC>>生化試劑>> (Rac)-NSC305787 hydrochloride | MCE
CAS | 53868-26-1 | 純度 | 99.07% |
---|---|---|---|
分子量 | 481.89 | 分子式 | C??H??Cl?N?O |
供貨周期 | 現貨 | 規格 | 5 mg |
貨號 | HY-18931A | 應用領域 | 醫療衛生,化工,生物產業,制藥/生物制藥 |
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CAS No. : 53868-26-1
產品活性:NSC305787 hydrochloride is an inhibitor of ezrin with a Kd of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC50 of 8.3 μM, has antitumor activity.
研究領域:Others
作用靶點:Others
In Vitro: NSC305787 hydrochloride is an inhibitor of ezrin with a Kd of 5.85 μM, and has antitumor activity. NSC305787 inhibits PKCΙ phosphorylation of Ezrin, Moesin, Radixin, MBP, with IC50s of 8.3, 9.4, 55, 58.9 μM, respectively. NSC305787 binds to PKCΙ with a Kd 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.
In Vivo: 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+p53fl/flpRBfl/fl) and shows a more favorable pharmacokinetic profile compared with NSC668394 in the mouse model.
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