Camptothecin
(Synonyms: 喜树碱; Campathecin; (S)-(+)-Camptothecin; CPT) 目录号 : GC15439
Camptothecin是一种特异性DNA拓扑异构酶I（Top1）抑制剂，IC50值为679 nM。
Cas No.:7689-03-4
Sample solution is provided at 25 µL, 10mM.
Camptothecin is a specific DNA topoisomerase I (Top1) inhibitor with an IC50 value of 679 nM[1]. Camptothecin is a plant alkaloid that induces DNA breaks and protein-DNA crosslinks[2]. Camptothecin has potent antitumor activity against colorectal, breast, lung and ovarian cancers[3].
In vitro, treatment of breast cancer-derived cells with high TOP1 enzyme activity (luminal subtype MCF7 and HER2 subtype HCC1419) with camptothecin (0.1-5µM) for 72h significantly inhibited cell viability with IC50 values of 0.089μM and 0.067μM, respectively[4]. Treatment of HeLa and HEK293 cells with camptothecin (0.5µM) for 8-24h significantly reduced the accumulation of hypoxia-inducible factor-1α (HIF-1α) but did not affect HIF-1β levels[5].
In vivo, oral treatment of obese mice with camptothecin (1 mg/kg) for 30 days induced the expression and secretion of growth differentiation factor 15 (GDF15) in the liver of mice, thereby reducing food intake, normalizing body weight and reversing metabolic dysfunction[6]. Camptothecin (2 mg/kg) treated mice with melanoma cell metastasis and significantly reduced the number of lung metastases[7].
References:
[1]Luzzio M J, Besterman J M, Emerson D L, et al. Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I[J]. Journal of medicinal chemistry, 1995, 38(3): 395-401.
[2]Stingele J, Jentsch S. DNA–protein crosslink repair[J]. Nature reviews Molecular cell biology, 2015, 16(8): 455-460.
[3]Huang Q, Wang L, Lu W. Evolution in medicinal chemistry of E-ring-modified Camptothecin analogs as anticancer agents[J]. European journal of medicinal chemistry, 2013, 63: 746-757.
[4]Tesauro C, Simonsen A K, Andersen M B, et al. Topoisomerase I activity and sensitivity to camptothecin in breast cancer-derived cells: a comparative study[J]. BMC cancer, 2019, 19: 1-15.
[5]Bertozzi D, Marinello J, Manzo S G, et al. The natural inhibitor of DNA topoisomerase I, camptothecin, modulates HIF-1α activity by changing miR expression patterns in human cancer cells[J]. Molecular cancer therapeutics, 2014, 13(1): 239-248.
[6]Lu J F, Zhu M Q, Xie B C, et al. Camptothecin effectively treats obesity in mice through GDF15 induction[J]. PLoS Biology, 2022, 20(2): e3001517.
[7]Schön M, Wienrich B G, Kneitz S, et al. KINK-1, a novel small-molecule inhibitor of IKKβ, and the susceptibility of melanoma cells to antitumoral treatment[J]. Journal of the National Cancer Institute, 2008, 100(12): 862-875.
Camptothecin是一种特异性DNA拓扑异构酶I（Top1）抑制剂，IC50值为679 nM[1]。Camptothecin是一种植物生物碱，诱导DNA断裂和蛋白质-DNA交联[2]。Camptothecin对结直肠癌、乳腺癌、肺癌和卵巢癌具有强大的抗肿瘤活性[3]。
在体外，Camptothecin（0.1-5µM）处理高TOP1酶活性的乳腺癌衍生细胞（管腔亚型MCF7和HER2亚型HCC1419）72h，显著抑制了细胞活力，IC50值分别为0.089μM和0.067μM[4]。Camptothecin（0.5µM）处理HeLa和HEK293细胞8-24h，显著减少了缺氧诱导因子-1α（HIF-1α）蓄积，但不影响HIF-1β水平[5]。
在体内，Camptothecin（1mg/kg）通过口服治疗肥胖小鼠30天，诱导小鼠肝脏表达和分泌生长分化因子15（GDF15），从而减少食物摄入量，使体重正常化并逆转了代谢功能障碍[6]。Camptothecin（2mg/kg）治疗黑色素瘤细胞转移的小鼠，显著减少了肺部转移灶数量[7]。
| Cell experiment [1]: | |
Cell lines | MCF7 (Luminal subtype)、HCC1419 (HER2 subtype) cells |
Preparation Method | Cells were seeded into 96-well flat-bottom plates with 100 μl of growth medium. After 24 h, the cell culture medium was replaced with medium alone, DMSO medium, or Camptothecin medium (at concentrations ranging from 0.1μM to 5μM) and incubated for 72 h. |
Reaction Conditions | 0.1-5µM; 72h |
Applications | High TOP1 enzymatic activity MCF7(Luminal subtype) and HCC1419(HER2 subtype) show high sensitivity toward camptothecin treatment, exhibiting the IC50 values of 0.089 μM and 0.067 μM, respectively. |
| Animal experiment [2]: | |
Animal models | Male Gfral+/+ and Gfral−/− mice |
Preparation Method | Mice at 8 weeks of age were maintained on HFD for 5 weeks. Each mouse received Camptothecin (1mg/kg) by gavage daily for 30 days, and their body weight and food intake were monitored every 3 days. |
Dosage form | 1mg/kg; p.o. |
Applications | Camptothecin induces hepatic expression and secretion of GDF15 in mice, which reduces food intake and thereby normalizing body weight and reversing metabolic dysfunctions in obese mice. |
References: [1]Tesauro C, Simonsen A K, Andersen M B, et al. Topoisomerase I activity and sensitivity to camptothecin in breast cancer-derived cells: a comparative study[J]. BMC cancer, 2019, 19: 1-15. [2]Lu J F, Zhu M Q, Xie B C, et al. Camptothecin effectively treats obesity in mice through GDF15 induction[J]. PLoS Biology, 2022, 20(2): e3001517. | |
| Cas No. | 7689-03-4 | SDF | |
| 别名 | 喜树碱; Campathecin; (S)-(+)-Camptothecin; CPT | ||
| 化学名 | (S)-4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione | ||
| Canonical SMILES | O=C(N(CC1=CC(C=CC=C2)=C2N=C13)C3=C4)C(CO5)=C4[C@@](O)(CC)C5=O | ||
| 分子式 | C20H16N2O4 | 分子量 | 348.35 |
| 溶解度 | ≥ 8.7mg/mL in DMSO | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8707 mL | 14.3534 mL | 28.7068 mL |
| 5 mM | 0.5741 mL | 2.8707 mL | 5.7414 mL |
| 10 mM | 0.2871 mL | 1.4353 mL | 2.8707 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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