tcsc1049 Campathecin

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Product Description

Campathecin is a potent DNA enzyme topoisomerase I inhibitor, with an IC50 of 679 nM.

IC50 & Target: IC50: 679 nM (topoisomerase I)[3]

In Vitro: [3H]BrCPT labeling of topoisomerase I is enhanced greatly by the presence of DNA; very little labeling of isolated topoisomerase I or isolated DNA occurrs. Even in the presence of DNA, [3H]BrCPT labeling of topoisomerase I is inhibited by camptothecin, suggesting that both CPT and BrCPT bind to the same site on the DNA-topoisomerase I binary complex[1]. With increasing concentrations of camptothecin, closed circular pRR322 DNA (form I) is converted to nicked circular DNA (form 11). This apparent nicking activitv of camptothecin required DNA topoisomerase I[2].

Information

CAS No7689-03-4
FormulaC20H16N2O4
Clinical Informationclinicalinformation
PathwayAntibody-drug Conjugate/ADC Related
Anti-infection
Apoptosis
Cell Cycle/DNA Damage
Epigenetics
TargetADC Cytotoxin
Antibiotic
Apoptosis
Fungal
Influenza Virus
MicroRNA
Topoisomerase

Specifications

Purity / Grade99.58%
SolubilityDMSO : 6.25 mg/mL (17.94 mM; Need ultrasonic)
SmilesO=C1C2=C([C@@](O)(CC)C(OC2)=O)C=C(N1C3)C(C3=C4)=NC5=C4C=CC=C5

Misc Information

Storage Instruction2-8°C, protect from light
Alternative NamesCampathecin; (S)-(+)-Camptothecin; CPT
Observed Molecular Weight348.35
References[1]. Luzzio MJ, et al. Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I. Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.
[2]. Bertozzi D, et al. The natural inhibitor of DNA topoisomerase I, camptothecin, modulates HIF-1α activity by changing miR expression patterns in human cancer cells. Mol Cancer Ther. 2014;13(1):239-248.
[3]. Schön M, et al. KINK-1, a novel small-molecule inhibitor of IKKbeta, and the susceptibility of melanoma cells to antitumoral treatment. J Natl Cancer Inst. 2008;100(12):862-875..
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