BPR1K653 - CAS 1192754-07-6
Catalog number:
1192754-07-6
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
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Description:
SBPR1K653 is a potent Aurora kinase inhibitor with potential anticancder activity. BPR1K653 specifically inhibited the activity of Aurora-A and Aurora-B kinase at low nano-molar concentrations in vitro. BPR1K653 was potent in targeting a variety of cancer cell lines regardless of the tissue origin, p53 status, or expression of MDR1. At the cellular level, BPR1K653 induced endo-replication and subsequent apoptosis in both MDR1-negative and MDR1-positive cancer cells. Importantly, it showed potent activity against the growth of xenograft tumors of the human cervical carcinoma KB and KB-derived MDR1-positive KB-VIN10 cells in nude mice. Finally, BPR1K653 also exhibited favorable pharmacokinetic properties in rats., BPR1K653 is a promising anti-cancer compound that has potential for the management of various malignancies, particularly for patients with MDR1-related drug resistance after prolonged chemotherapeutic treatments.
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Purity:
0.98
Synonyms:
BPR1K653; BPR1K 653; BPR1K-653
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Current Developer:
National Health Research Institutes, Taiwan
1.BPR1K653, a novel Aurora kinase inhibitor, exhibits potent anti-proliferative activity in MDR1 (P-gp170)-mediated multidrug-resistant cancer cells.
Cheung CH1, Lin WH, Hsu JT, Hour TC, Yeh TK, Ko S, Lien TW, Coumar MS, Liu JF, Lai WY, Shiao HY, Lee TR, Hsieh HP, Chang JY. PLoS One. 2011;6(8):e23485. doi: 10.1371/journal.pone.0023485. Epub 2011 Aug 24.
BACKGROUND: Over-expression of Aurora kinases promotes the tumorigenesis of cells. The aim of this study was to determine the preclinical profile of a novel pan-Aurora kinase inhibitor, BPR1K653, as a candidate for anti-cancer therapy. Since expression of the drug efflux pump, MDR1, reduces the effectiveness of various chemotherapeutic compounds in human cancers, this study also aimed to determine whether the potency of BPR1K653 could be affected by the expression of MDR1 in cancer cells.
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CAS 1192754-07-6 BPR1K653

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