产品说明书

OTS514

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Chemical Structure| 1338540-63-8 同义名 : -
CAS号 : 1338540-63-8
货号 : A265446
分子式 : C21H20N2O2S
纯度 : 99%+
分子量 : 364.461
MDL号 : MFCD29924710
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(288.1 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

PO 0.5% CMC-Na 37 mg/mL suspension

生物活性
描述 TOPK (T-lymphokine-activated killer cell-originated protein kinase) is highly and frequently transactivated in various cancer tissues, including lung and triple-negative breast cancers, and plays an indispensable role in the mitosis of cancer cells. OTS514 is an extremely potent TOPK inhibitor. The compound inhibited TOPK kinase activity with a median inhibitory concentration (IC50) value of 2.6 nM. After a 2-hour incubation with 0.2 μM OTS514, the highest inhibition was observed for TOPK (83.5% inhibition) out of a panel of 60 diverse human protein kinases indicating the specificity of the TOPK inhibitory effect of this compound. In a xenograft model of A549 cells (TOPK-positive lung cancer cells), intravenous administration of free OTS514 at 1, 2.5, and 5 mg/kg once a day for 2 weeks resulted in TGI (tumor growth inhibition) of 5.7, 43.3, and 65.3% on day 15, respectively, without any body weight loss. Further, a significant increase in the megakaryocyte population was observed after treatment with 20 or 40 nM OTS514 (P = 0.04 and P = 0.02, respectively). Moreover, OTS514 was administered to mice bearing LU-99 cancer cells after the tumor size reached about 200 mm3. Intravenous administration of OTS514 (5 mg/kg) once a day for 2 weeks achieved good growth-suppressive effect with TGI of 104% without any body weight loss[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.74mL

0.55mL

0.27mL

13.72mL

2.74mL

1.37mL

27.44mL

5.49mL

2.74mL
参考文献

[1]Matsuo Y, Park JH, 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]TOPK Inhibitor Induces Complete Tumor Regression in Xenograft Models of Human Cancer Through Inhibition of Cytokinesis