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β-拉帕醌 /β-Lapachone {[allProObj[0].p_purity_real_show]}

货号:A951815 同义名: beta-拉帕醌 / ARQ-501;NSC-26326 Ambeed 开学季,买赠积分,赢豪礼

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).

β-Lapachone 化学结构 CAS号:4707-32-8
β-Lapachone 化学结构
CAS号:4707-32-8
β-Lapachone 3D分子结构
CAS号:4707-32-8
β-Lapachone 化学结构 CAS号:4707-32-8
β-Lapachone 3D分子结构 CAS号:4707-32-8
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β-Lapachone 纯度/质量文件 产品仅供科研

货号:A951815 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Topo I Topo II Topo IV Topoisomerase 其他靶点 纯度
Ellagic acid {[allProObj[0].p_purity_real_show]}
β-Lapachone {[allProObj[0].p_purity_real_show]}
(s)-10-hydroxycamptothecin {[allProObj[0].p_purity_real_show]}
Camptothecin ++

Topo I, IC50: 0.68 μM

{[allProObj[0].p_purity_real_show]}
Betulinic acid ++

Eukaryotic topoisomerase I, IC50: 5 μM

{[allProObj[0].p_purity_real_show]}
Topotecan ++++

Topo I (DU-145 Luc cells), IC50: 2 nM

Topo I (MCF-7 Luc cells), IC50: 13 nM

{[allProObj[0].p_purity_real_show]}
Irinotecan HCl Trihydrate {[allProObj[0].p_purity_real_show]}
SN-38 {[allProObj[0].p_purity_real_show]}
Levofloxacin hydrate {[allProObj[0].p_purity_real_show]}
Dexrazoxane {[allProObj[0].p_purity_real_show]}
Ofloxacin {[allProObj[0].p_purity_real_show]}
Enoxacin {[allProObj[0].p_purity_real_show]}
Flumequine +

Topo II, IC50: 15 μM

{[allProObj[0].p_purity_real_show]}
Levofloxacin {[allProObj[0].p_purity_real_show]}
Etoposide {[allProObj[0].p_purity_real_show]}
Pefloxacin mesylate dihydrate {[allProObj[0].p_purity_real_show]}
Marbofloxacin {[allProObj[0].p_purity_real_show]}
Voreloxin HCl {[allProObj[0].p_purity_real_show]}
Mitoxantrone dihydrochloride PKC {[allProObj[0].p_purity_real_show]}
Nalidixic acid {[allProObj[0].p_purity_real_show]}
Doxorubicin {[allProObj[0].p_purity_real_show]}
Novobiocin sodium {[allProObj[0].p_purity_real_show]}
Amonafide {[allProObj[0].p_purity_real_show]}
Pirarubicin {[allProObj[0].p_purity_real_show]}
Idarubicin HCl +++

Topo II (MCF-7 cells), IC50: 3.3 ng/mL

{[allProObj[0].p_purity_real_show]}
Genistein EGFR {[allProObj[0].p_purity_real_show]}
Teniposide {[allProObj[0].p_purity_real_show]}
Moxifloxacin {[allProObj[0].p_purity_real_show]}
Ciprofloxacin {[allProObj[0].p_purity_real_show]}
Clinafloxacin {[allProObj[0].p_purity_real_show]}
Gatifloxacin {[allProObj[0].p_purity_real_show]}
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

{[allProObj[0].p_purity_real_show]}
Epirubicin HCl {[allProObj[0].p_purity_real_show]}
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。

β-Lapachone 生物活性

靶点
  • Topo I

描述 β-Lapachone functions as a topoisomerase I inhibitor. At a concentration of 25 μM, β-Lapachone inhibits camptothecin-induced DNA cleavage [1]. Lapachone (at concentrations ranging from 10 to 40 μM) significantly diminishes the colony-forming ability of CHO cells and demonstrates cytotoxicity during the S phase. Additionally, β-Lapachone induces substantial DNA strand breaks in CHO cells at concentrations exceeding 10 μM [2]. β-Lapachone (10 μM) inhibits JCPyV replication in IMR-32 cells. β-Lapachone at 1.0 μM significantly impacts JCPyV propagation in JCI cells. Moreover, β-Lapachone at concentrations ranging from 0.01 to 0.1 μM inhibits VP1 production in JCI cells [4].
体内研究

β-Lapachone (0.066%) mitigates cisplatin-induced renal injury, and its combination with cisplatin enhances this effect in mice. Additionally, β-Lapachone increases the expression of the Mre11-Rad50-Nbs1 (MRN) complex in mice [3].

体外研究

β-Lapachone functions as a topoisomerase I inhibitor. At a concentration of 25 μM, β-Lapachone inhibits camptothecin-induced DNA cleavage [1].

Lapachone (at concentrations ranging from 10 to 40 μM) significantly diminishes the colony-forming ability of CHO cells and demonstrates cytotoxicity during the S phase. Additionally, β-Lapachone induces substantial DNA strand breaks in CHO cells at concentrations exceeding 10 μM [2].

β-Lapachone (10 μM) inhibits JCPyV replication in IMR-32 cells. β-Lapachone at 1.0 μM significantly impacts JCPyV propagation in JCI cells. Moreover, β-Lapachone at concentrations ranging from 0.01 to 0.1 μM inhibits VP1 production in JCI cells [4].

β-Lapachone 动物研究

Dose 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)
Administration p.o., i.v., i.p.
Pharmacokinetics
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
AUC0→last 3.602 μg·h/ml (p.o.)
1.149 μg·h/ml (i.v.)
T1/2 11.36 h (p.o.)
2.45 h (i.v.)
Tmax 6 h (p.o.)
Cmax 0.218 μg/ml (p.o.)
7.133 μg/ml (i.v.)
AUC0→∞ 4.866 μg·h/ml (p.o.)
1.174 μg·h/ml (i.v.)

β-Lapachone 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 -

β-Lapachone 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.13mL

0.83mL

0.41mL

20.64mL

4.13mL

2.06mL

41.28mL

8.26mL

4.13mL

β-Lapachone 技术信息

CAS号4707-32-8
分子式C15H14O3
分子量 242.27
别名 beta-拉帕醌 ;ARQ-501;NSC-26326;SL 11001;NSC 629749;Beta-Lapachone
运输蓝冰
存储条件

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 25 mg/mL(103.19 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

无水乙醇: 8 mg/mL(33.02 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

动物实验配方
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