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Lucanthone

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Chemical Structure| 479-50-5 同义名 : 硫坎酮
CAS号 : 479-50-5
货号 : A737309
分子式 : C20H24N2OS
纯度 : 99%+
分子量 : 340.482
MDL号 : MFCD00866726
存储条件:

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 25 mg/mL(73.43 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 APE1 is an enzyme that is involve in the DNA base excision repair pathway. Its main role in the repair of damaged or mismatched nucleotides in DNA is to create a nick in the phosphodiester backbone of the AP site created when DNA glycosylase removes the damaged base[1]. Lucanthone is a novel autophagic inhibitor which also inhibits APE1by direct protein binding without affecting its redox activity. It induces apoptosis via cathepsin D accumulation and enhance histone deacetylase inhibitor-induced cell death in MDA-MB-231 cells. Combined treatment with lucanthone and TRAIL significantly induced apoptosis in human renal carcinoma, prostate carcinoma and lung carcinoma cells[2]. Lucanthone reduces cell viability to a similar extent in a panel of seven breast cancer cell lines. In addition, a direct comparison reveals that Lucanthone is significantly more potent than Chloroquine (CQ) at reducing breast cancer cell viability with a mean IC50 of 7.2 μM versus 66 μM for CQ[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
NCT02014545 Brain Metastases ... 展开 >> Non-small Cell Lung Cancer 收起 << Phase 2 Withdrawn(Pending resolution o... 展开 >>f study drug issues) 收起 << - United States, North Carolina ... 展开 >> Comprehensive Cancer Center of Wake Forest University Winston-Salem, North Carolina, United States, 27157 收起 <<
NCT01587144 Glioblastoma Multiforme Phase 2 Terminated(Sponsor's decision) - United States, California ... 展开 >> UCSD Moores Cancer Center La Jolla, California, United States, 92093 UCI Medical Center Orange, California, United States, 92868 United States, New York Dent Neurologic Institute Amherst, New York, United States, 14226 United States, Ohio Fairview Hospital Moll Cancer Center/Cleveland Clinic Cleveland, Ohio, United States, 44111 Cleveland Clinic Cleveland, Ohio, United States, 44195 Hillcrest Hospital Hirsh Cancer Center/Cleveland Clinic Mayfield, Ohio, United States, 44124 India Gujarat Cancer Research Institute Ahmedabad, Gujarat, India, 380016 Jaslok Hospital & Research Centre Mumbai, Maharashtra, India, 400062 Bhagwan Mahaveer Cancer Hospital & Reseach Centre Jaipur, Rajasthan, India, 302017 Chittaranjan National Cancer Institute Kolkata, West Bengal, India, 700026 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.94mL

0.59mL

0.29mL

14.69mL

2.94mL

1.47mL

29.37mL

5.87mL

2.94mL

参考文献

[1]Whitaker AM, Freudenthal BD. APE1: A skilled nucleic acid surgeon. DNA Repair (Amst). 2018 Nov;71:93-100.

[2]Yoon JY, Woo SM, Seo SU, Song SR, Lee SG, Kwon TK. Lucanthone, Autophagy Inhibitor, Enhances the Apoptotic Effects of TRAIL through miR-216a-5p-Mediated DR5 Upregulation and DUB3-Mediated Mcl-1 Downregulation. Int J Mol Sci. 2021 Dec 21;23(1):17.

[3]Carew JS, Espitia CM, Esquivel JA 2nd, Mahalingam D, Kelly KR, Reddy G, Giles FJ, Nawrocki ST. Lucanthone is a novel inhibitor of autophagy that induces cathepsin D-mediated apoptosis. J Biol Chem. 2011 Feb 25;286(8):6602-13.