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CAS No.: 4707-32-8

β-拉帕醌 Catalog No. CSN12283

Synonyms: ARQ-501;NSC-26326;NSC629749

β-Lapachone is a naturally occurring quinone obtained from the bark of the lapacho tree (Tabebuia avellanedae) with cancer chemopreventive properties and a potent inhibitor of IDO1 (IC50=0.44 μM).

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述β-Lapachone, a plant product, can inhibit the formation of cleavable complex through a direct interaction with topoisomerase I, unlike camptothecin which stabilizes the cleavable complex. Incubation of topoisomerase I with β-Lapachone before adding DNA substrate, but not post incubation of topoisomerase I with DNA or treatment of DNA with beta-lapachone before topoisomerase, could dramatically increase topoisomerase I-mediated DNA cleavage induced by camptothecin. A dose-dependent decrease of MCF-7 cell survival and increase of cell apoptosis could be observed 4 days post treatment with β-Lapachone at concentration ranging in 1-10μM for 48h. Decrease of hyperphosphorylated forms of Rb and cleavage of Lamin B could be observed in MCF-7 cells treated with 5μM β-Lapachone for >3h. Besides inhibition of topoisomerase I, β-Lapachone also exhibited effect on several other targets or pathways. U937 cells pretreated with β-Lapachone showed inhibition of TNF-induced NF-kB activation, p65 translocation, IκBα degradation, and NF-κB-dependent reporter gene expression, as well as LPS-induced NF-kB activation. TNF-induced activation of AP-1, c-Jun N-terminal kinase, MAPKK, caspase-3, as well as cytotoxicity could be abolished by β-Lapachone. β-Lapachone triggered apoptosis signaling JNK (but not p38 or ERK1/2) and subsequent CPP32/Yama activation mediated by the generation of ROS.

动物研究

剂量

Rat: 40 mg/kg^[3] (p.o.); 1.5 mg/kg^[3] (i.v.) Mice: 5 mg/kg^[4] (i.v.); 70 mg/kg - 80 mg/kg^[4] (p.o.); 1.25 mg/kg - 5 mg/kg^[5] (i.p.), 50 mg/kg^[6] (i.p., BID)

给药途径

p.o., i.v., i.p.

动物药代数据

Animal	Rats^[3]
Dose	40 mg/kg (p.o., 0 - 24h) 1.5 mg/kg (i.v., 0 - 12h)
Administration	p.o., i.v.
F	0.1554
AUC_0→last	3.602 μg·h/ml (p.o.) 1.149 μg·h/ml (i.v.)
T_1/2	11.36 h (p.o.) 2.45 h (i.v.)
T_max	6 h (p.o.)
C_max	0.218 μg/ml (p.o.) 7.133 μg/ml (i.v.)
AUC_0→∞	4.866 μg·h/ml (p.o.) 1.174 μg·h/ml (i.v.)

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
NCT03575078 Lymphoma Phase 1 Not yet recruiting August 23, 2023 -
参考文献

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03575078	Lymphoma	Phase 1	Not yet recruiting	August 23, 2023	-

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.1276 mL
- 20.6381 mL
- 41.2763 mL
- 5 mM
- 0.8255 mL
- 4.1276 mL
- 8.2553 mL
- 10 mM
- 0.4128 mL
- 2.0638 mL
- 4.1276 mL

技术信息

CAS号

4707-32-8

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H14O3

运输

蓝冰

分子量

242.27

别名

ARQ-501;NSC-26326;NSC629749;SL 11001;beta-lapachone;beta-拉帕醌;β-拉帕醌;β-拉帕酮

溶解度

DMSO	100.0 mg/mL (412.8 mM)
Water	insoluble

动物实验配方

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