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OTS514 {[allProObj[0].p_purity_real_show]}

货号:A265446 Ambeed 开学季,买赠积分,赢豪礼

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 化学结构
CAS号:1338540-63-8
OTS514 3D分子结构
CAS号:1338540-63-8
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]}
批次查询: 批次纯度:

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产品名称 MEK MEK1 MEK1/2 MEK2 MEK5 其他靶点 纯度
Honokiol {[allProObj[0].p_purity_real_show]}
Mirdametinib ++++

MEK, IC50: 0.33 nM

{[allProObj[0].p_purity_real_show]}
Binimetinib +++

MEK, IC50: 12 nM

{[allProObj[0].p_purity_real_show]}
BI-847325 ++

MEK1, IC50: 25 nM

+++

MEK2, IC50: 4 nM

{[allProObj[0].p_purity_real_show]}
U0126-EtOH +

MEK1, IC50: 0.07 μM

++

MEK2, IC50: 0.06 μM

{[allProObj[0].p_purity_real_show]}
GDC-0623 ++++

MEK1, IC50: 0.13 nM

{[allProObj[0].p_purity_real_show]}
TAK-733 ++++

MEK1, IC50: 3.2 nM

{[allProObj[0].p_purity_real_show]}
Trametinib ++++

MEK1, IC50: 0.92 nM

++++

MEK2, IC50: 1.8 nM

{[allProObj[0].p_purity_real_show]}
Selumetinib +++

MEK1, Kd: 99 nM

MEK1, IC50: 14 nM

+

MEK2, Kd: 530 nM

{[allProObj[0].p_purity_real_show]}
CI-1040 ++

MEK1, IC50: 17 nM

++

MEK2, IC50: 17 nM

{[allProObj[0].p_purity_real_show]}
Myricetin {[allProObj[0].p_purity_real_show]}
Refametinib ++

MEK1, IC50: 19 nM

++

MEK2, IC50: 47 nM

{[allProObj[0].p_purity_real_show]}
Cobimetinib +++

MEK1, IC50: 4.2 nM

{[allProObj[0].p_purity_real_show]}
PD98059 +

MEK1, IC50: 2 μM

{[allProObj[0].p_purity_real_show]}
SL327 +

MEK1, IC50: 0.18 μM

+

MEK2, IC50: 0.22 μM

AP-1 {[allProObj[0].p_purity_real_show]}
PD318088 {[allProObj[0].p_purity_real_show]}
AZD8330 +++

MEK1/2, IC50: 7 nM

{[allProObj[0].p_purity_real_show]}
Pimasertib {[allProObj[0].p_purity_real_show]}
(E/Z)-BIX02189 ++++

MEK5, IC50: 1.5 nM

{[allProObj[0].p_purity_real_show]}
(E/Z)-BIX02188 +++

MEK5, IC50: 4.3 nM

{[allProObj[0].p_purity_real_show]}
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

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

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