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COTI-2 {[allProObj[0].p_purity_real_show]}

货号:A703883

COTI-2是一种口服可用的硫代半胱氨酸酮(thiosemicarbazone)衍生物,具有激活突变 p53 的作用,具有潜在的抗肿瘤活性。

COTI-2 化学结构 CAS号:1039455-84-9
COTI-2 化学结构
CAS号:1039455-84-9
COTI-2 3D分子结构
CAS号:1039455-84-9
COTI-2 化学结构 CAS号:1039455-84-9
COTI-2 3D分子结构 CAS号:1039455-84-9
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COTI-2 纯度/质量文件 产品仅供科研

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产品名称 p53 其他靶点 纯度
Pifithrin-μ 99%+
Pifithrin-α HBr 98%
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。

COTI-2 生物活性

描述 COTI-2, distinguished as a low-toxicity anticancer agent, is an orally bioavailable third-generation p53 activator that can reactivate mutant forms of p53 and concurrently inhibit the PI3K/AKT/mTOR signaling pathway. It has been shown to trigger apoptosis across various human tumor cell lines and possesses antitumor properties in head and neck squamous cell carcinoma (HNSCC) through both p53-dependent and independent mechanisms, effectively restoring mutant p53 to a wild-type structure[1].[2].[3].
体内研究

Furthermore, COTI-2 prominently suppresses tumor growth in HT-29 human colorectal tumor xenografts at a dosage of 10 mg/kg, effectively reducing tumor sizes at specific intervals post-treatment and extending the period for tumors to reach certain sizes. Remarkably, COTI-2 also significantly curtails tumor growth in the SHP-77 small cell lung cancer (SCLC) xenograft model with doses as minimal as 3 mg/kg. In treatments involving U87-MG tumors, COTI-2 not only shrinks tumor volumes at designated times after treatment but also prolongs the duration needed for the growth of U87-MG xenografts in nude mice[2].

体外研究

After 72 hours of treatment with COTI-2, there's a notable inhibition in the proliferation rates across all examined cell lines, including COLO-205, HCT-15, and SW620, demonstrating significant antiproliferative effects. COTI-2 also displays activity against several human glioblastoma cell lines, including U87-MG, SNB-19, SF-268, and SF-295, at relatively low concentrations. In SHP-77 cells treated with COTI-2 at approximate IC50 concentrations, early apoptosis is induced in 40 to 47% of the total cells[2].

COTI-2 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02433626 Ovarian Cancer ... 展开 >> Fallopian Tube Cancer Endometrial Cancer Cervical Cancer Peritoneal Cancer Head and Neck Cancer HNSCC 收起 << Phase 1 Recruiting December 2018 United States, Illinois ... 展开 >> Northwestern Memorial Hospital Recruiting Chicago, Illinois, United States Contact: Wilberto Nieves-Neira, MD    312-472-4684       Principal Investigator: Wilberto Nieves-Neira, MD          United States, Texas MD Anderson Cancer Centre Recruiting Houston, Texas, United States Contact: Shannon Westin, MD    713-794-4314       Principal Investigator: Shannon Westin, MD 收起 <<

COTI-2 参考文献

[1]Duffy MJ, et al. Mutant p53 as a target for cancer treatment. Eur J Cancer. 2017 Sep;83:258-265.

[2]Salim KY, et al. COTI-2, a novel small molecule that is active against multiple human cancer cell lines in vitro and in vivo. Oncotarget. 2016 Jul 5;7(27):41363-41379.

[3]Lindemann A, et al. COTI-2, A Novel Thiosemicarbazone Derivative, Exhibits Antitumor Activity in HNSCC through p53-dependent and -independent Mechanisms. Clin Cancer Res. 2019 Sep 15;25(18):5650-5662.

COTI-2 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.73mL

0.55mL

0.27mL

13.64mL

2.73mL

1.36mL

27.29mL

5.46mL

2.73mL

COTI-2 技术信息

CAS号1039455-84-9
分子式C19H22N6S
分子量 366.483
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

溶解方案

DMSO: 4 mg/mL(10.91 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
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