拓扑异构酶抑制剂(PNU-159682)

中文名	PNU-159682
英文名	PNU-159682
别名	蒽环类新霉素化合物PNU-159682 拓扑异构酶抑制剂(PNU-159682)
英文别名	PNU159682 PNU-159682
CAS	202350-68-3
化学式	C32H35NO13
分子量	641.62
密度	1.58±0.1 g/cm3(Predicted)
沸点	838.5±65.0 °C(Predicted)
溶解度	10毫米DMSO
酸度系数	7.34±0.60(Predicted)
存储条件	under inert gas (nitrogen or Argon) at 2–8 °C
体外研究	PNU-159682 (0-500 nM; 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 IC 70 values are 0.577 nM, 0.39 nM, 0.128 nM, and 0.081 nM, 0.086 nM and 0.075 nM for HT-29, A2780, DU145, EM-2, Jurkat and CEM cells, respectively. It against human tumor cell lines with IC 70 in the ranging 68 nM-578 nM and 181 nM-1717 nM 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, Granta-519, SuDHL4.Luc, and WSU-DLCL2 with IC 50 values of 0.10 nM, 0.020 nM, 0.055 nM, and 0.1 nM, respectively. While MMAE is against BJAB.Luc, Granta-519, SuDHL4.Luc, and WSU-DLCL2 with IC 50 values of 0.54 nM, 0.25 nM, 1.19 nM and 0.25 nM, respectively.PNU-159682 is thousands of times more cytotoxic than doxorubicin and can be used to develop a new class of ADCs. PNU159682toanti-CD22antibody (anti-CD22-NMS249) exhibits strong anti-tumor effects in vitro . Anti-CD22-NMS249 (PNU159682toanti-CD22antibody) 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 IC 50 values of 0.058 nM, 0.030 nM, 0.0221 nM, and 0.01 nM, respectively.PNU-159682 (100 μM) weakly inhibits topoisomerase II unknotting activity. PNU-159682 shows cytotoxic effect on CAIX-expressing SKRC-52 cells with IC 50 of 25 nM. Cell Viability Assay Cell Line: HT-29, A2780, DU145, EM-2, Jurkat and CEM cells Concentration: 0-500 nM 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 IC 70 values of PNU-159682 are in the subnanomolar range (0.07-0.58 nM) and noticeably lower than that recorded for both MMDX and doxorubicin.
体内研究	PNU-159682 (single-dose; i.v.15 μg/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 90 μg/kg MMDX (increase in life=36%).PNU-159682 (i.v. 4 μg/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. PNU159682toanti-CD22antibody (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: 4 μg/kg Administration: Intravenous injection; q7dx3; 40 days Result: Exhibited anti-cancer effects in MX-1 human mammary carcinoma xenografts to PNU-159682.

拓扑异构酶抑制剂(PNU-159682) - 配置溶液浓度参考

	1mg	5mg	10mg
1 mM	1.559 ml	7.793 ml	15.586 ml
5 mM	0.312 ml	1.559 ml	3.117 ml
10 mM	0.156 ml	0.779 ml	1.559 ml
5 mM	0.031 ml	0.156 ml	0.312 ml

最后更新：2024-01-02 23:10:35

拓扑异构酶抑制剂(PNU-159682) - 简介

PNU-159682是一种化学物质，具有以下性质：

外观：PNU-159682是一种固体物质，可能呈现为粉末或结晶形态。
解离常数：PNU-159682的解离常数也未知。

PNU-159682的用途和应用范围是未知的，没有公开的文献和信息提供详细的用途说明。

PNU-159682的制备方法：

没有详细信息和文献引用，不清楚PNU-159682的制备方法和合成路径。

在处理和使用PNU-159682时，注意以下安全信息：

毒性：无法获取详细信息，不能确定PNU-159682的毒性和危险性。
接触和吸入：任何化学物质都应该避免皮肤直接接触和吸入。
环境：化学品的处理和处置应符合环境保护要求。
遵循实验室安全操作规程：在处理任何化学物质时，始终要遵循实验室安全操作规程，并使用适当的个人防护装备（如实验手套、防护眼镜和实验室通风设备）。

最后更新：2024-04-09 22:09:11

上海吉至生化科技有限公司

现货供应

产品名: PNU-159682 去供应商网站查看询盘
CAS: 202350-68-3
产地: 中国上海
包装: 5mg
规格: 95%
价格: 7498.00
库存: 现货
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产品描述: 中文名：PNU-159682 英文名:PNU-159682 CAS:202350-68-3 规格:95% 产地:中国上海

上海麦克林生化科技股份有限公司

现货供应

产品名: PNU-159682 去供应商网站查看询盘
CAS: 202350-68-3
产地: 上海
规格: P880712
价格: 25mg-1606,5mg-364,1mg-98
库存: 7天内发货
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上海源叶生物科技有限公司

产品名: PNU-159682 去供应商网站查看询盘
CAS: 202350-68-3
产地: 上海
规格: 95%
价格: 1mg 2800,5mg 6100,10mg 9700,25mg 17100,50mg 29300
电话: 18301782025
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