Camptothecin (Synonyms: MAGCPT, NSC 94600) |
| رقم الكتالوجGC15439 |
Camptothecin (CPT) ، وهو نوع من القلويد ، هو مثبط DNA topoisomerase I (Topo I) مع IC50 من 679 نانومتر
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Cas No.: 7689/3/4
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.
| 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. | 7689/3/4 | SDF | |
| المرادفات | MAGCPT, NSC 94600 | ||
| Chemical Name | (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 | ||
| Formula | C20H16N2O4 | M.Wt | 348.35 |
| الذوبان | ≥ 8.7mg/mL in DMSO | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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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- Purity: >98.00%
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