PNU-159682

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Chemical Structure| 202350-68-3 同义名 : -
CAS号 : 202350-68-3
货号 : A158340
分子式 : C32H35NO13
纯度 : 99%+
分子量 : 641.62
MDL号 : MFCD12756329
存储条件:

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(163.65 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
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
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

[1]Quintieri L, et al. Formation and antitumor activity of PNU-159682, a major metabolite of nemorubicin in human liver microsomes. Clin Cancer Res. 2005 Feb 15;11(4):1608-17.

[2]Cazzamalli S, et al. Acetazolamide Serves as Selective Delivery Vehicle for Dipeptide-Linked Drugs to Renal Cell Carcinoma. Mol Cancer Ther. 2016 Dec;15(12):2926-2935.

[3]Pengxuan Zhao, et al. Recent advances of antibody drug conjugates for clinical applications. Acta Pharm Sin B. 2020 Sep;10(9):1589-1600.

[4]Joanne Lundy, Interim data: Phase I/IIa study of EGFR-targeted EDV nanocells carrying cytotoxic drug PNU-159682 (E-EDV-D682) with immunomodulatory adjuvant EDVs carrying α-galactosyl ceramide (EDV-GC) in patients with recurrent, metastatic pancreatic cancer. GASTROINTESTINAL CANCER—GASTROESOPHAGEAL, PANCREATIC, AND HEPATOBILIARY