OTS514 hydrochloride

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

OTS514 hydrochloride 

OTS5144 hydrochloride 是一种高效的 TOPK 抑制剂，IC50 为 2.6 nM。OTS514 hydrochloride 强效抑制 TOPK 阳性的肿瘤细胞生长。OTS514 hydrochloride 诱导细胞周期停滞和凋亡 (apoptosis)。

OTS514 hydrochloride

OTS514 hydrochloride Chemical Structure

CAS No. : 2319647-76-0

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OTS514 hydrochloride 的其他形式现货产品:

OTS514

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[1]. OTS514 hydrochloride induces cell cycle arrest and apoptosis[2].

IC50 & Target

IC50: 2.6 nM (TOPK)[1]
体外研究
(In Vitro)

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[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: Human myeloma cell lines (MM1.S, MM1.R, RPMI 8226, 8226Dox40, KMS34, KMS34CFZ, KMS11, JJN3, LP-1, NCI H929, U266B1)
Concentration: 1.5625, 3.125, 6.25, 12.5, 25, 50, and 100 nM
Incubation Time: 72 hours
Result: 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, was resistant.

体内研究
(In Vivo)

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)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/cSLC-nu/nu mice bearing a xenograft model of A549 cells[1]
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.

分子量

400.92

Formula

C21H21ClN2O2S
CAS 号

2319647-76-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Matsuo Y, et al. TOPK inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition of cytokinesis. Sci Transl Med. 2014 Oct 22;6(259):259ra145.

    [2]. Stefka AT, et al. Potent anti-myeloma activity of the TOPK inhibitor OTS514 in pre-clinical models. Cancer Med. 2020 Jan;9(1):324-334.

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