生物活性 | |||
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描述 | PNU-159682 demonstrates profound cytotoxic effects on various human tumor cell lines, as revealed through the sulforhodamine B assay. The IC70 values showcase its potent activity, ranging from 0.081 nM to 0.577 nM against cell lines such as HT-29, A2780, DU145, EM-2, Jurkat, and CEM, indicating a high degree of cytotoxic efficiency[1]. When compared to other therapeutic agents like MMDX and doxorubicin, PNU-159682's efficacy remains superior, with IC70 values spanning from 68 nM to 578 nM against MMDX, and even broader ranges of 181 nM to 1717 nM towards doxorubicin, emphasizing its potency[1]. In cell viability assays against non-Hodgkin lymphoma (NHL) cell lines, PNU-159682's potency again surpasses that of MMAE, with IC50 values as low as 0.020 nM, compared to MMAE's IC50 values which are significantly higher[2]. This trend continues in vitro with anti-CD22 antibody conjugates (anti-CD22-NMS249), where PNU-159682 enhances the efficacy of these antibody-drug conjugates (ADCs), yielding IC50 values that are 2 to 20 times more potent than pinatuzumab vedotin against similar NHL cell lines[3]. Moreover, PNU-159682 demonstrates a marginal inhibition of topoisomerase II and specific cytotoxicity towards CAIX-expressing SKRC-52 cells, with an IC50 of 25 nM, suggesting a potential for targeting specific cancer markers[4]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.56mL 0.31mL 0.16mL |
7.79mL 1.56mL 0.78mL |
15.59mL 3.12mL 1.56mL |
参考文献 |
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