Camptothecin
Catalog No.: GC15439Purity:>98.00%Synonyms: MAGCPT, NSC 94600
Camptothecin is a specific DNA topoisomerase I (Top1) inhibitor with an IC50 value of 679 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 7689-03-4
10mM (in 1mL DMSO)In Stock
$35.00
1
250mgIn Stock
$34.00
1
500mgIn Stock
$65.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $35.00 | In Stock | 1 | |
| 250mg | $34.00 | In Stock | 1 | |
| 500mg | $65.00 | In Stock | 1 |
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Citations
1 publicationsPublications from researchers using this productDescription
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.
Protocol
| Cell experiment [1]: | |
|
Cell lines |
MCF7 (Luminal subtype)、HCC1419 (HER2 subtype) cells |
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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]: | |
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Animal models |
Male Gfral+/+ and Gfral−/− mice |
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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. |
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Dosage form |
1mg/kg; p.o. |
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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. |
|
Product Documents
Purity:>98.00%Appearance:A solid
Biological Data
1 / 1
Chemical Properties
CAS No.
7689-03-4
Synonyms
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
SMILES
O=C(N(CC1=CC(C=CC=C2)=C2N=C13)C3=C4)C(CO5)=C4[C@@](O)(CC)C5=O
Molecular Formula
C20H16N2O4
Molecular Weight
348.35
Solubility
10mg/mL in 1M NaOH;6.7mg/mL in DMSO
Storage
4°C, protect from light
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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