产品
编 号：F638859
分子式：C21H21ClN2O2S
分子量：400.92
分子式：C21H21ClN2O2S
分子量：400.92
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CAS No: 2319647-76-0
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生物活性：
OTS514 hydrochloride is a highly potent TOPK inhibitor, which inhibits TOPK kinase activity with a median inhibitory concentration (IC50) value of 2.6 nM. OTS514 hydrochloride strongly suppresses the growth of TOPK-positive cancer cells. OTS514 hydrochloride induces cell cycle arrest and apoptosis.
体内研究：
OTS514 (1-5 mg/kg; once a day for 2 weeks; intravenous administration) induces tumor regression in a xenograft model of A549 cells (TOPK-positive lung cancer cells).Animal Model:Female BALB/cSLC-nu/nu mice bearing a xenograft model of A549 cells
Dosage:1, 2.5, and 5 mg/kg
Administration:Intravenously treated; once every day for 2 weeks
Result:Resulted in tumor growth inhibition (TGI) of 5.7, 43.3, and 65.3% on day 15, respectively, without any body weight loss.
体外研究：
OTS514 (1.5625-100 nM) induces cell cycle arrest and apoptosis at nanomolar concentrations in a series of human myeloma cell lines (HMCL) and prevents outgrowth of a putative CD138+ stem cell population from multiple myeloma (MM) patient-derived peripheral blood mononuclear cells.
OTS514 hydrochloride is a highly potent TOPK inhibitor, which inhibits TOPK kinase activity with a median inhibitory concentration (IC50) value of 2.6 nM. OTS514 hydrochloride strongly suppresses the growth of TOPK-positive cancer cells. OTS514 hydrochloride induces cell cycle arrest and apoptosis.
体内研究：
OTS514 (1-5 mg/kg; once a day for 2 weeks; intravenous administration) induces tumor regression in a xenograft model of A549 cells (TOPK-positive lung cancer cells).Animal Model:Female BALB/cSLC-nu/nu mice bearing a xenograft model of A549 cells
Dosage:1, 2.5, and 5 mg/kg
Administration:Intravenously treated; once every day for 2 weeks
Result:Resulted in tumor growth inhibition (TGI) of 5.7, 43.3, and 65.3% on day 15, respectively, without any body weight loss.
体外研究：
OTS514 (1.5625-100 nM) induces cell cycle arrest and apoptosis at nanomolar concentrations in a series of human myeloma cell lines (HMCL) and prevents outgrowth of a putative CD138+ stem cell population from multiple myeloma (MM) patient-derived peripheral blood mononuclear cells.
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