货号:A951815 同义名: beta-拉帕醌 / ARQ-501;NSC-26326
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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产品名称 | Topo I ↓ ↑ | Topo II ↓ ↑ | Topo IV ↓ ↑ | Topoisomerase ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Ellagic acid | ✔ | 98% | |||||||||||||||||
β-Lapachone | ✔ | 99%+ | |||||||||||||||||
(s)-10-hydroxycamptothecin | ✔ | 98+% | |||||||||||||||||
Camptothecin |
++
Topo I, IC50: 0.68 μM |
98% | |||||||||||||||||
Betulinic acid |
++
Eukaryotic topoisomerase I, IC50: 5 μM |
98% | |||||||||||||||||
Topotecan |
++++
Topo I (MCF-7 Luc cells), IC50: 13 nM Topo I (DU-145 Luc cells), IC50: 2 nM |
98% | |||||||||||||||||
Irinotecan HCl Trihydrate | ✔ | 98% | |||||||||||||||||
SN-38 | ✔ | 98% | |||||||||||||||||
Levofloxacin hydrate | ✔ | 98% | |||||||||||||||||
Dexrazoxane | ✔ | 99%+ | |||||||||||||||||
Ofloxacin | ✔ | 98+% | |||||||||||||||||
Enoxacin | ✔ | 99%+ | |||||||||||||||||
Flumequine |
+
Topo II, IC50: 15 μM |
98% | |||||||||||||||||
Levofloxacin | ✔ | 97% | |||||||||||||||||
Etoposide | ✔ | 98% | |||||||||||||||||
Pefloxacin mesylate dihydrate | ✔ | 99+% | |||||||||||||||||
Marbofloxacin | ✔ | 98+% | |||||||||||||||||
Voreloxin HCl | ✔ | 98% | |||||||||||||||||
Mitoxantrone dihydrochloride | ✔ | PKC | 98% | ||||||||||||||||
Nalidixic acid | ✔ | 98% | |||||||||||||||||
Doxorubicin | ✔ | 98% | |||||||||||||||||
Novobiocin sodium | ✔ | 95% | |||||||||||||||||
Amonafide | ✔ | 99%+ | |||||||||||||||||
Pirarubicin | ✔ | 98%+ | |||||||||||||||||
Idarubicin HCl |
+++
Topo II (MCF-7 cells), IC50: 3.3 ng/mL |
99%+ | |||||||||||||||||
Genistein | ✔ | EGFR | 98% | ||||||||||||||||
Teniposide | ✔ | 98% | |||||||||||||||||
Moxifloxacin | ✔ | 98% | |||||||||||||||||
Ciprofloxacin | ✔ | 98% | |||||||||||||||||
Clinafloxacin | ✔ | 97% | |||||||||||||||||
Gatifloxacin | ✔ | 98% | |||||||||||||||||
Daunorubicin HCl |
+++
DNA synthesis, Ki: 20 nM |
98% | |||||||||||||||||
Epirubicin HCl | ✔ | 99%+ | |||||||||||||||||
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。 |
靶点 |
|
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]. |
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 |
|
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 | - |
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 |
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 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Room Temperature |
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 |