OTS514 | TOPK Inhibitor | AmBeed-信号通路专用抑制剂

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OTS514 {[allProObj[0].p_purity_real_show]}

货号：A265446

OTS514 is a highly potent TOPK inhibitor with an IC50 value of 2.6 nM.

OTS514 化学结构
CAS号：1338540-63-8

OTS514 3D分子结构
CAS号：1338540-63-8

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OTS514 纯度/质量文件产品仅供科研

货号：A265446 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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MEK 亚型比较

产品名称	MEK ↓ ↑	MEK1 ↓ ↑	MEK1/2 ↓ ↑	MEK2 ↓ ↑	MEK5 ↓ ↑	其他靶点	纯度
Honokiol	✔						98%
Mirdametinib	++++ MEK, IC50: 0.33 nM						99%+
Binimetinib	+++ MEK, IC50: 12 nM						99%+
BI-847325		++ MEK1, IC50: 25 nM		+++ MEK2, IC50: 4 nM			99%+
U0126-EtOH		+ MEK1, IC50: 0.07 μM		++ MEK2, IC50: 0.06 μM			98%
GDC-0623		++++ MEK1, IC50: 0.13 nM					99%+
TAK-733		++++ MEK1, IC50: 3.2 nM					99%+
Trametinib		++++ MEK1, IC50: 0.92 nM		++++ MEK2, IC50: 1.8 nM			99%+
Selumetinib		+++ MEK1, Kd: 99 nM MEK1, IC50: 14 nM		+ MEK2, Kd: 530 nM			99%+
CI-1040		++ MEK1, IC50: 17 nM		++ MEK2, IC50: 17 nM			99%+
Myricetin		✔					98%
Refametinib		++ MEK1, IC50: 19 nM		++ MEK2, IC50: 47 nM			99%+
Cobimetinib		+++ MEK1, IC50: 4.2 nM					99%+
PD98059		+ MEK1, IC50: 2 μM					99%+
SL327		+ MEK1, IC50: 0.18 μM		+ MEK2, IC50: 0.22 μM		AP-1	98+%
PD318088			✔				98%
AZD8330			+++ MEK1/2, IC50: 7 nM				99%+
Pimasertib							98%
(E/Z)-BIX02189					++++ MEK5, IC50: 1.5 nM		99%+
(E/Z)-BIX02188					+++ MEK5, IC50: 4.3 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

OTS514 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].

OTS514 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

OTS514 实验方案

计算器

存储液制备

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

OTS514 技术信息

CAS号	1338540-63-8
分子式	C₂₁H₂₀N₂O₂S
分子量	364.461

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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

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OTS514 {[allProObj[0].p_purity_real_show]}

OTS514 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

OTS514 质控信息

OTS514 生物活性

OTS514 参考文献

OTS514 实验方案

OTS514 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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热门区域

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C

F

G

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OTS514 纯度/质量文件产品仅供科研