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PNU-159682  ≥98%

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包装规格：1mg 5mg 10mg 25mg 50mg in glass bottle
溶解性：溶于DMSO（≥ 100 mg/mL）
产品描述：基本信息 产品编号： P10707  产品名称： PNU-159682 CAS: 202350-68-3   储存条件 粉末 2-8℃ 四年     分子式： C32H35NO13 溶于液体 -80℃ 6个月 分子量 641.62 -20℃ 1个月 化学名：  PNU-159682;3'-deamino-3'',4'-anhydro-[2''(S)-methoxy-3''(R)-oxy-4''-morpholinyl]doxorubicin Solubility (25°C)：   体外:   DMSO 100 mg/mL (155.86mM; Need ultrasonic) Water   Ethanol   体内(现配现用): 1.请依序添加每种溶剂： 10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility: ≥ 2.5 mg/mL (3.90mM); Clear solution 此方案可获得 ≥ 2.5 mg/mL (3.90mM，饱和度未知) 的澄清溶液。 以 1mL 工作液为例，取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400μL PEG300 中，混合均匀；向上述体系中加入50μL Tween-80，混合均匀；然后继续加入 450μL生理盐水定容至 1mL。 2.请依序添加每种溶剂： 10% DMSO→90% (20% SBE-β-CD in saline) Solubility: 2.5 mg/mL (3.90mM); Suspended solution; Need ultrasonic 此方案可获得 2.5 mg/mL (3.90mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1mL 工作液为例，取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3.请依序添加每种溶剂： 10% DMSO→90% corn oil Solubility: ≥ 2.5 mg/mL (3.90mM); Clear solution 此方案可获得 ≥ 2.5 mg/mL (3.90mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1mL 工作液为例，取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900μL玉米油中，混合均匀。 ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 1.5586mL 7.7928mL 15.5855mL 5mM 0.3117mL 1.5586mL 3.1171mL 10mM 0.1559mL 0.7793mL 1.5586mL   生物活性 产品描述 蒽环类新霉素代谢产物的代谢产物，是一种 DNA 拓扑异构酶 I (Topo I) 抑制剂，具有出色的细胞毒性。 靶点 Daunorubicins/Doxorubicins Topoisomerase I 体外研究 PNU-159682 (0-500nM; exposed to the compounds for 1 hour and then cultured in compound-free medium for 72 hours) has cytotoxic effects on human tumor cell lines in a sulforhodamine B assay. The IC70 values are 0.577nM, 0.39nM, 0.128nM, and 0.081nM, 0.086nM and 0.075nM for HT-29, A2780, DU145, EM-2, Jurkat and CEM cells, respectively. It against human tumor cell lines with IC70 in the ranging 68 nM-578nM and 181 nM-1717nM towards MMDX and doxorubicin, respectively . PNU-159682 is more potent than MMAE on NHL cell lines. In a cell viability assay, PNU-159682 is against BJAB.Luc, Granta519, SuDHL4.Luc, and WSU-DLCL2 with IC50 values of 0.10nM, 0.020nM, 0.055nM, and 0.1nM, respectively. While MMAE is against BJAB.Luc, Granta-519, SuDHL4.Luc, and WSU-DLCL2 with IC50 values of 0.54nM, 0.25nM, 1.19nM and 0.25nM, respectively . PNU-159682 is thousands of times more cytotoxic than doxorubicin and can be used to develop a new class of ADCs. PNU159682 to anti-CD22 antibody (anti-CD22-NMS249) exhibits strong anti-tumor effects in vitro. Anti-CD22-NMS249 (PNU159682 to anti-CD22 antibody) is active in in vitro viability assays of NHL cell lines and is 2 to 20 fold more potent than pinatuzumab vedotin, the ADC anti-CD22-NMS249 is against BJAB.Luc, Granta-519, SuDHL4.Luc, and WSU-DLCL2 with IC50 values of 0.058nM, 0.030nM, 0.0221nM, and 0.01nM, respectively. PNU-159682 (100μM) weakly inhibits topoisomerase II unknotting activity. PNU-159682 shows cytotoxic effect on CAIXexpressing SKRC-52 cells with IC50 of 25nM. Cell Viability Assay Cell Line: HT-29, A2780, DU145, EM-2, Jurkat and CEM cells Concentration: 0-500nM Incubation Time: Exposed to the PNU-159682 for 1 hour and then cultured in compound-free medium for 72 hours Result: Was 2,360- to 790-fold and 6,420- to 2,100-fold more potent than MMDX and doxorubicin, respectively.Exhibited IC70 values of PNU-159682 are in the subnanomolar range (0.07-0.58nM) and noticeably lower than that recorded for both MMDX and doxorubicin. 体内研究 PNU-159682 (single-dose; i.v.15μg/kg) is a maximum tolerated dose in murine L1210 leukemia model. PNU-159682 shows an improved antitumor activity in vivo. The antitumor effect of PNU-159682 (increase in life span=29%) is comparable to that afforded by 90μg/kg MMDX (increase in life=36%).PNU-159682 (i.v. 4μg/kg; q7dx3; 40 days) has a therapeutic response in MX-1 human mammary carcinoma mice. What’s more, from day 39, four out of seven mice receiving PNU-159682 exhibits complete tumor regression.PNU-159682 is more cytotoxic than doxorubicin and can be used to develop a new class of ADCs. PNU159682 to anti-CD22 antibody (anti-CD22-NMS249) exhibits strong anti-tumor effects in vivo. ADC dose (anti-CD22-NMS249; 50 µg/m2 conjugated PNU-159682) is well tolerated in mice and results in less than 10% weight loss.In the BJAB.Luc model the efficacy of antiCD22-NMS249 (single dose; 2 mg/kg) is similar to anti-CD22-vc-MMAE. At 2 mg/kg dosage, antiCD22-NMS249 gives complete remission of the tumors (NMS249: 110-134%TGI vs. vc-MMAE: 114-143%TGI). Additionally, a single dose of antiCD22-NMS249 at 2 mg/kg results in tumor stasis for three weeks Animal Model: Four- to six-week-old female CD-1 athymic nude mice with MX-1 tumor fragments Dosage: 4μg/kg Administration: Intravenous injection; q7dx3; 40 days Result: Exhibited anti-cancer effects in MX-1 human mammary carcinoma xenografts to PNU-159682.
保存条件：2-8℃ 充氮保存

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