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OTS964 HCl {[allProObj[0].p_purity_real_show]}

货号:A217615 同义名: OTS-964;OTS964 (hydrochloride) Ambeed 开学季,买赠积分,赢豪礼

OTS-964 is a TOPK (T-LAK cell originated protein kinase) inhibitor with IC50 value of 28 nM, which can specifically block cytokinesis, leading to apoptosis, in a broad range of cancer cells.

OTS964 HCl 化学结构 CAS号:1338545-07-5
OTS964 HCl 化学结构
CAS号:1338545-07-5
OTS964 HCl 3D分子结构
CAS号:1338545-07-5
OTS964 HCl 化学结构 CAS号:1338545-07-5
OTS964 HCl 3D分子结构 CAS号:1338545-07-5
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OTS964 HCl 纯度/质量文件 产品仅供科研

货号:A217615 标准纯度: {[allProObj[0].p_purity_real_show]}
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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

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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

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TAK-733 ++++

MEK1, IC50: 3.2 nM

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Trametinib ++++

MEK1, IC50: 0.92 nM

++++

MEK2, IC50: 1.8 nM

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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

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

MEK1, IC50: 19 nM

++

MEK2, IC50: 47 nM

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Cobimetinib +++

MEK1, IC50: 4.2 nM

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PD98059 +

MEK1, IC50: 2 μM

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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

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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。

OTS964 HCl 生物活性

靶点
  • TOPK

    TOPK, IC50:28 nM

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. OTS-964 is a potent TOPK inhibitor with high affinity and selectivity for TOPK kinase with IC50 value of 28 nM. OTS964 (2 μM) could inhibit 79.7% of TOPK activity, whereas the mean and the SD of the inhibitory effects against other kinases were 18.5 and 24.6%, respectively. OTS964 inhibited the growth of TOPK-positive cells with low IC50 values [A549 (31 nM), LU-99 (7.6 nM), DU4475 (53 nM), MDA-MB-231 (73 nM), T47D (72 nM), Daudi (25 nM), UM-UC-3 (32 nM), HCT-116 (33 nM), MKN1 (38 nM), MKN45 (39 nM), HepG2 (19 nM), MIAPaca-2 (30 nM), and 22Rv1 (50 nM)]. In mice bearing LU-99 lung cancer cells, a TGI (tumor growth inhibition) of 44% was observed on day 22 without any body weight loss after intravenous treatment of OTS964 at 40 mg/kg. A TGI of 110% was observed on day 22 after treatment of liposomal OTS964 at 40 mg/kg. The U-99 xenograft mice were intravenously treated with liposomal OTS964 (40 mg/kg) or vehicle at days 1, 4, 8, and 11, and tumors were collected on day 12. Treatment with OTS964 significantly increased the number of LU-99 cells with the “intercellular bridge” (P < 0.0001), which is one of the markers indicating impaired cell division. The oral administration of free OTS964 at 50 or 100 mg/kg once every day for 2 weeks resulted in TGIs of 79 and 113% on day 15, respectively, without any body weight loss in LU-99 xenograft model[2].

OTS964 HCl 参考文献

[1]Ikeda Y, Park JH, et al. T-LAK Cell-Originated Protein Kinase (TOPK) as a Prognostic Factor and a Potential Therapeutic Target in Ovarian Cancer. Clin Cancer Res. 2016 Dec 15;22(24):6110-6117.

[2] Matsuo Y, Park JH, Miyamoto T, et al. TOPK inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition of cytokinesis. Sci Transl Med. 2014;6(259):259ra145.

OTS964 HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.66mL

2.33mL

1.17mL

23.31mL

4.66mL

2.33mL

OTS964 HCl 技术信息

CAS号1338545-07-5
分子式C23H25ClN2O2S
分子量 428.975
别名 OTS-964;OTS964 (hydrochloride);OTS964 hydrochloride
运输蓝冰
存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 85 mg/mL(198.15 mM),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

H2O: 2 mg/mL(4.66 mM),配合低频超声,并水浴加热至45℃助溶

动物实验配方
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