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DNA Damage/DNA Repair Topoisomerase (S)-(+)-Camptothecin

(S)-(+)-Camptothecin

Catalog No. T1123   CAS 7689-03-4
Synonyms: CPT, Campathecin, Camptothecin, NSC-100880
Purity 99.87% Datasheet

(S)-(+)-Camptothecin is a specific inhibitor of DNA topoisomerase I (Topo I), isolated from Camptotheca acuminata.

(S)-(+)-Camptothecin, CAS 7689-03-4
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Biological Description
Chemical Properties
Storage & Solubility Information
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Description (S)-(+)-Camptothecin is a specific inhibitor of DNA topoisomerase I (Topo I), isolated from Camptotheca acuminata.
Targets&IC50 Topo I :ic50 0.68μM,  
Kinase Assay Topoisomerase I Cleavable Complex Assay: Topoisomerase I is isolated from calf thymus and is devoid of topoisomerase II. All reactions are carried out in 10 mL volumes of reaction buffer (50 mM Tris-HCl, pH 7.5, 100 mM KCl, 0.5 mM EDTA, and 30 pg/mL BSA) in microtiter plates. Camptothecin is dissolved in DMSO at 10 mg/mL and serially diluted in 96-well microtiter plates to which the 32P end-labeled pBR322 DNA and topoisomerase enzyme are added. The reaction mixture is incubated at room temperature for 30 min and then the reaction stopped by adding 2 mL of a mixture of sodium dodecyl sulfate and proteinase K (1.6% and 0.14 mg/mL final concentrations, respectively). The plates are heated at 50 °C for 30 min, 10 mL of standard stop mixture containing 0.45 N NaOH is added in order to generate single-stranded DNA, and the samples are electrophoresed in 1.5% agarose gels in TBE buffer. Gels are blotted on nitrocellulose paper, dried, and exposed to X-ray film. The units of cleavage are calculated from the autoradiographs and plotted against the log drug concentration. The IC50 values are then obtaine
Cell Research
Tumor cells are plated in 100 μL of medium in 96-well microtiter plates at a density of 1500 to 4000 cells per well and allowed to adhere overnight. Cells are incubated with Camptothecin for 48 hours and then with fresh medium for 48 hours. Camptothecin at each concentration is added in quadruplicate. Following a 4-hour incubation of treated cells with MTT, the reduced dye product is extracted from the cells with 0.2 mL of DMSO followed by 50 μL of Sorensen's buffer. The plates are shaken briefly, and the absorbance at 570 nm is read and quantitated. Curves are fitted to the MTT assay data using a four-parameter logistic equation.(Only for Reference)
Cell lines: U87MG, A549 and H838 cells
Animal Research
Animal Model: Nude mice (NIH-I high fertility strain) bearing xenografts of CASE, SW48, DOY, SPA, and CLO cells
Synonyms CPT, Campathecin, Camptothecin, NSC-100880
Purity 99.87%
Appearance solid
Molecular Weight 348.36
Formula C20H16N2O4
CAS No. 7689-03-4

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 8.6 mM

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL

Citations

References and Literature
1. Wall ME, et al. J Am Chem Soc, 1966, 88 (16), 3888–3890. 2. Luzzio MJ, et al. J Med Chem, 1995, 38(3), 395-401. 3. Giovanella BC, et al. Cancer Res, 1991, 51(11), 3052-3055. 4. Hentze H, et al. Hepatology, 2004, 39(5), 1311-1320. 5. Cheng F, et al. Oncogene, 2011, 30(33), 3599-3611.

Related Compound Libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Natural Compound Library for HTS Anti-cancer Compound Library Clinical Compound Library Selected Plant-sourced Compound Library DNA Damage & Repair Compound Library Anti-cancer Clinical Compound Library Cardiotoxicity Compound Library Killers Collection

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