化合物PNU-159682 T16557

Product Introduction
Bioactivity


英文名: PNU-159682

描述: PNU-159682 是蒽环类新霉素的代谢产物，是一种 DNA 拓扑异构酶 II 抑制剂，具有出色的细胞毒性。

体外活性: PNU-159682 inhibits a panel of human tumor cell lines (IC70 values in the range of 0.07-0.58 nM). PNU-159682 is 2,360- to 790-fold and 6,420- to 2,100-fold more potent than MMDX and doxorubicin, respectively. PNU-159682 displays cytotoxic effect on CAIX-expressing SKRC-52 cells (IC50: 25 nM). PNU-159682 (10 μM)-DNA adducts contain one or two drug molecules bound to double-stranded DNA. PNU-159682 (100 μM) weakly inhibits topoisomerase II unknotting activity [1][2][3].

体内活性: PNU-159682 (25 nmol/kg) shows an effective antitumor effect in mice bearing SKRC-52 xenografted tumors. PNU-159682 (15 μg/kg, i.v.) displays antitumor activity in mice bearing disseminated murine L1210 leukemia and in MX-1 human mammary carcinoma xenografts at 4 μg/kg[1][3].

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

溶解度: DMSO : 96.7 mg/mL (150.71 mM)


关键字: PNU 159682 | inhibit | non-Hodgkin’s lymphoma | PNU159682 | ADCs Toxin | acute myeloid leukemia | ADC Payload | EDV nanocell | AML | Inhibitor | ADC Cytotoxin | Topoisomerase | NMS249 | NHL | PNU-159682

相关产品: Doxorubicin | Zoliflodacin | (4-NH2)-Exatecan | Podofilox | Norfloxacin | Mitoxantrone dihydrochloride | Topoisomerase inhibitor 2 | Exatecan mesylate dihydrate | Razoxane | Cholesteryl Hemisuccinate

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途