货号:A159794 同义名: Campathecin;CPT
Camptothecin (CPT) 是一种生物碱,作为 DNA 拓扑异构酶 I (Topo I) 抑制剂,IC50 为 679 nM。它对结直肠癌、乳腺癌、肺癌和卵巢癌表现出强效的抗肿瘤活性,并通过改变人类癌细胞中的微小 RNA (miRNA) 表达模式来调节缺氧诱导因子 1α (HIF-1α) 活性。
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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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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 | Camptothecin (CPT), an alkaloid, acts as an inhibitor for DNA topoisomerase I (Topo I) with an IC50 value of 679 nM[1]. Demonstrating significant antitumor effects on colorectal, breast, lung, and ovarian cancers, CPT also affects the activity of hypoxia-inducible factor-1α (HIF-1α) by altering the patterns of microRNAs (miRNA) expression in human cancer cells[2].[3]. |
体内研究 | Administering Camptothecin (2 mg/kg every other day) to mice presenting extensive pulmonary metastases resulted in a significant reduction of these metastases when combined with the kinase inhibitor of nuclear factor-kappaB-1 (KINK-1)[5]. |
体外研究 | MCF7 (Luminal subtype) and HCC1419 (HER2 subtype) cells, characterized by elevated TOP1 enzyme activity, are particularly susceptible to Camptothecin treatment (ranging from 0.1 μM to 5 μM over 72 hours), showing IC50 values of 0.089 μM and 0.067 μM, respectively[4]. A dosage of Camptothecin at 0.5 μM for 6 and 24 hours notably decreases the expression of VEGF activated by desferrioxamine. Furthermore, Camptothecin administration (0.5 μM; 8 to 24 hours) effectively inhibits the accumulation of HIF-1α induced by desferrioxamine[2]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
A2780 | cytotoxicity assay | IC50=4 nM | 11858737 | ||
A427 | ~1 μM | Growth inhibitory assay | IC50=24 nM | 9876111 | |
A549 | cytotoxicity assay | IC50=67 nM | 10841808 | ||
A549 | cytotoxicity assay | IC50=14 nM | 11334569 | ||
Dose | Rat: 30 mg/kg[3] (i.g.) | ||||||||||||||||||
Administration | i.g. | ||||||||||||||||||
Pharmacokinetics |
|
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.87mL 0.57mL 0.29mL |
14.35mL 2.87mL 1.44mL |
28.71mL 5.74mL 2.87mL |
CAS号 | 7689-03-4 |
分子式 | C20H16N2O4 |
分子量 | 348.352 |
别名 | Campathecin;CPT;(+)-Camptothecin;20(S)-Camptothecine;d-Camptothecin;Camptothecine;NSC 94600;MAG-CPT;(S)-(+)-Camptothecin |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Sealed in dry,Room Temperature |
溶解度 |
DMSO: 5 mg/mL(14.35 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 1M NaOH: 10 mg/mL(28.71 mM),配合低频超声,并调节pH至11 |
动物实验配方 |