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COTI-2

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Chemical Structure| 1039455-84-9 同义名 : -
CAS号 : 1039455-84-9
货号 : A703883
分子式 : C19H22N6S
纯度 : 98%
分子量 : 366.483
MDL号 : MFCD28502211
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

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：
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].
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 <<
实验方案
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
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.