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Beta-Lapachone

β-兰帕科恩,β-拉帕醌,ARQ501,β-Lapachone,ARQ 501,ARQ-501,

Beta-Lapachone是一种选择性的DNA topoisomerase I（DNA拓扑异构酶I）抑制剂，对DNA拓扑异构酶II或连接酶无抑制作用。

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生物活性

Beta-Lapachone is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2.
体外研究
体内研究
激酶实验
细胞实验

0.005 - 50 μM
动物实验

25-50 mg/kg 腹腔给药
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Li CJ, et al. J Biol Chem. 1993, 268(30), 22463-22468.

分子式 C15H14O3	分子量 242.27	CAS号 4707-32-8	储存方式 ﹣20 ℃冷藏长期储存。冰袋运输
溶剂（常温）	DMSO >25 mg/mL	Water <1 mg/mL	Ethanol 20 mg/mL

体内溶解度

NCT Number	Conditions	Interventions	Sponsor/Collaborators	Phases	Start Date	Last Updated
NCT00622063	Cancer	Drug: ARQ 501	ArQule	Phase 1\|Phase 2	2006-12-01	2013-02-22
NCT00099190	Carcinoma	Drug: ARQ 501	ArQule	Phase 1	2004-12-01	2009-04-27
NCT00524524	Advanced Solid Tumors	Drug: ARQ 501	ArQule	Phase 1	2007-08-01	2011-10-17
NCT00358930	Head and Neck Neoplasms\|Carcinoma, Squamous Cell	Drug: ARQ 501	ArQule	Phase 2	2006-07-01	2009-04-27
NCT00102700	Pancreatic Cancer\|Adenocarcinoma	Drug: ARQ 501 in combination with gemcitabine	ArQule	Phase 2	2005-01-01	2009-04-28
NCT00075933	Cancer	Drug: ARQ 501	ArQule	Phase 1	2003-09-01	2009-04-27
NCT00310518	Cancer	Drug: ARQ 501	ArQule	Phase 2	2006-02-01	2009-04-28
NCT01502800	Solid Tumors	Drug: ARQ 761\|Drug: ARQ 761 Weekly Administration\|Drug: Bi-Weekly Administration of ARQ 761\|Drug: Two Consecutive Weeks Administration of ARQ 761 with one week of rest	University of Texas Southwestern Medical Center\|ArQule	Phase 1	2011-12-01	2016-06-07
NCT02514031	Pancreatic Cancer	Drug: ARQ-761\|Drug: Gemcitabine\|Drug: nab-paclitaxel	University of Texas Southwestern Medical Center	Phase 1	2015-10-01	2016-05-31
NCT01285388	Metabolic Syndrome\|Obesity	Drug: MB12066	KT&G Life Sciences Corp\|KT&G Corporation	Phase 1	2010-07-01	2011-01-26
NCT01444677	Metabolic Syndrome\|Obesity	Drug: MB12066\|Drug: MB12066\|Drug: MB12066\|Drug: MB12066\|Drug: Placebo	KT&G Life Sciences Corp\|KT&G Corporation	Phase 1	2011-04-01	2012-07-16

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。