OTS514 is a highly potent TOPK inhibitor with an IC50 of 2.6 nM. OTS514 strongly suppresses the growth of TOPK-positive cancer cells. OTS514 induces cell cycle arrest and apoptosis.
IC50&Target
IC50: 2.6 nM (TOPK)
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.
IC50 values ranged from 11.6 to 29.4 nM in parental cell lines, indicating a potent inhibitory effect. Only the RPMI 8226-Dox40 cell line, which overexpresses the multi-drug resistance transporter gene ABCB1, is resistant.
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.
分子式
C21H21ClN2O2S
分子量
364.46
CAS号
1338540-63-8
运输条件
Room temperature in continental US; may vary elsewhere.