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Karenitecin

Catalog No. T14703   CAS 203923-89-1
Synonyms: BNP 1350, Cositecan

Karenitecin (Cositecan) is an inhibitor of topoisomerase I. It has potent anti-cancer activity.

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Karenitecin Chemical Structure
Karenitecin, CAS 203923-89-1
Pack Size Availability Price/USD Quantity
25 mg 10-14 weeks $ 1,530.00
50 mg 10-14 weeks $ 1,990.00
100 mg 10-14 weeks $ 3,110.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Karenitecin (Cositecan) is an inhibitor of topoisomerase I. It has potent anti-cancer activity.
In vitro Karenitecin, a topoisomerase I inhibitor, exhibits potent anti-cancer properties by effectively inhibiting the growth of various human colon cancer cell lines, including COLO205, COLO320, LS174T, SW1398, and WiDr, demonstrated by IC50 values of 2.4 nM, 1.5 nM, 1.6 nM, 2.9 nM, and 3.2 nM, respectively[2]. Furthermore, it not only induces DNA damage in A253 cells at concentrations of 0.01, 0.07, and 0.7 μM but also elevates the levels of cyclin E and cdk2 proteins at 0.07 and 0.7 μM. Significant cell growth inhibition in A253 cells is achieved with IC10, IC50, and IC90 values of 0.01, 0.07, and 0.7 μM after a 2-hour treatment. Additionally, at low concentrations, Karenitecin significantly augments cyclin B/cdc2-associated kinase activity, whereas it slightly diminishes this activity at higher concentrations[1].
In vivo Karenitecin (1.0 mg/kg daily × 5 i.p.) significantly reduces growth in both parental Pgp-negative xenografts and Pgp-positive xenografts[2]. It demonstrates a maximum growth inhibition of 61% in COLO320 cells and 54% in COLO205 colon cancer cells following i.p. administration at a dosage of 1 mg/kg in mice.
Synonyms BNP 1350, Cositecan
Molecular Weight 448.59
Formula C25H28N2O4Si
CAS No. 203923-89-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Yin MB, et al. Characterization of protein kinase chk1 essential for the cell cycle checkpoint after exposure of human head and neck carcinoma A253 cells to a novel topoisomerase I inhibitor BNP1350. Mol Pharmacol. 2000 Mar;57(3):453-9. 2. Van Hattum AH, et al. New highly lipophilic camptothecin BNP1350 is an effective drug in experimental human cancer. Int J Cancer. 2000 Oct 15;88(2):260-6.

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Keywords

Karenitecin 203923-89-1 DNA Damage/DNA Repair Topoisomerase BNP 1350 BNP-1350 BNP1350 Cositecan inhibitor inhibit

 

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