購物車 
-
PNU-159682
- names：
PNU-159682
- CAS號：
202350-68-3
MDL Number： MFCD12756329 - MF(分子式)： C32H35NO13 MW(分子量)： 641.62
- EINECS:No data available Reaxys Number:No data available
- Pubchem ID:9874188 Brand:BIOFOUNT
PNU-159682(202350-68-3)是一種高效的蒽環類新霉素代謝產物 (DNA 拓撲異構酶 II 抑制劑)，PNU-159682具有突出的細胞毒性，是一種有效的 ADC 細胞毒素。
| 貨品編碼 | 規格 | 純度 | 價格 (￥) | 現價(￥) | 特價(￥) | 庫存描述 | 數量 | 總計 (￥) |
|---|---|---|---|---|---|---|---|---|
| YZM000908-5mg | 5mg | 96.8% | ￥ 7593.00 | ￥ 7593.00 | 2-3天 | ￥ 0.00 | ||
| YZM000908-1mg | 1mg | 96.8% | ￥ 3412.00 | ￥ 3412.00 | 2-3天 | ￥ 0.00 |
| 中文別名 | PNU-159682(202350-68-3),拓撲異構酶抑制劑(PNU-159682),PNU159682,PNU 159682 |
| 英文別名 | PNU-159682(202350-68-3),PNU159682,PNU 159682 |
| CAS號 | 202350-68-3 |
| Inchi | InChI=1S/C32H35NO13/c1-13-29-16(33-7-8-43-31(42-3)30(33)46-29)9-20(44-13)45-18-11-32(40,19(35)12-34)10-15-22(18)28(39)24-23(26(15)37)25(36)14-5-4-6-17(41-2)21(14)27(24)38/h4-6,13,16,18,20,29-31,34,37,39-40H,7-12H2,1-3H3/t13-,16-,18-,20-,29+,30+,31-,32-/m0/s1 |
| InchiKey | SLURUCSFDHKXFR-WWMWMSKMSA-N |
| 分子式 Formula | C32H35NO13 |
| 分子量 Molecular Weight | 641.62 |
| 溶解度Solubility | 生物體外In Vitro:DMSO溶解度≥ 100 mg/mL(155.86 mM)H2O< 0.1 mg/mL(insoluble)*"≥" means soluble可溶, but saturation unknown溶解度未知. |
| 性狀 | 粉紅色到紅色固體粉末 |
| 儲藏條件 Storage conditions | 4°C，在氮氣下儲存 |
PNU-159682(202350-68-3)實驗注意事項：
1.實驗前需戴好防護眼鏡，穿戴防護服和口罩，佩戴手套，避免與皮膚接觸。
2.實驗過程中如遇到有毒或者刺激性物質及有害物質產生，必要時實驗操作需要手套箱內完成以免對實驗人員造成傷害
3.實驗后產生的廢棄物需分類存儲，并交于專業生物廢氣物處理公司處理，以免造成環境污染
PNU-159682(202350-68-3) Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.
Tag:PNU-159682(202350-68-3),PNU-159682試劑,抑制劑PNU-159682,PNU-159682的純度,PNU-159682的作用,PNU-159682的合成,PNU-159682的MSDS,PNU-159682的溶解度,PNU-159682的外觀,PNU-159682的含量,PNU-159682的生產
| 產品說明 | PNU-159682(202350-68-3)是一種高效的蒽環類新霉素代謝產物 (DNA 拓撲異構酶 II 抑制劑)，PNU-159682具有突出的細胞毒性 |
| Introduction | PNU-159682(202350-68-3), a highly potent metabolite of the anthracycline nemorubicin (DNA topoisomerase II inhibitor) with outstanding cytotoxicity, is a potentADCs cytotoxin. |
| Application1 | |
| Application2 | |
| Application3 |
We recently demonstrated that nemorubicin (MMDX), an investigational antitumor drug, is converted to an active metabolite, PNU-159682, by human liver cytochrome P450 (CYP) 3A4. The objectives of this study were: (1) to investigate MMDX metabolism by liver microsomes from laboratory animals (mice, rats, and dogs of both sexes) to ascertain whether PNU-159682 is also produced in these species, and to identify the CYP form(s) responsible for its formation; (2) to compare the animal metabolism of MMDX with that by human liver microsomes (HLMs), in order to determine which animal species is closest to human beings; (3) to explore whether differences in PNU-159682 formation are responsible for previously reported species- and sex-related differences in MMDX host toxicity. The animal metabolism of MMDX proved to be qualitatively similar to that observed with HLMs since, in all tested species, MMDX was mainly converted to PNU-159682 by a single CYP3A form.
| 警示圖 | |
| 危險性 | warning |
| 危險性警示 | Not available |
| 安全聲明 | H303吞入可能有害+H313皮膚接觸可能有害+H2413吸入可能對身體有害 |
| 安全防護 | P264處理后徹底清洗+P280戴防護手套/穿防護服/戴防護眼罩/戴防護面具+P305如果進入眼睛+P351用水小心沖洗幾分鐘+P338取出隱形眼鏡（如果有）并且易于操作,繼續沖洗+P337如果眼睛刺激持續+P2393獲得醫療建議/護理 |
| 備注 | 實驗過程中防止吸入、食入，做好安全防護 |
The interaction of nemorubicin metabolite PNU-159682 with DNA fragments d(CGTACG)(2), d(CGATCG)(2) and d(CGCGCG)(2) shows a strong but reversible binding to G:C base pairs.
Mazzini S1, Scaglioni L, Mondelli R, Caruso M, Sirtori FR. Bioorg Med Chem. 2012 Dec 15;20(24):6979-88. doi: 10.1016/j.bmc.2012.10.033. Epub 2012 Nov 3.
The antitumor anthracycline nemorubicin is converted by human liver microsomes to a major metabolite, PNU-159682 (PNU), which was found to be much more potent than its parent drug toward cultured tumor cells and in vivo tumor models. The mechanism of action of nemorubicin appears different from other anthracyclines and until now is the object of studies. In fact PNU is deemed to play a dominant, but still unclear, role in the in vivo antitumor activity of nemorubicin. The interaction of PNU with the oligonucleotides d(CGTACG)(2), d(CGATCG)(2) and d(CGCGCG)(2) was studied with a combined use of (1)H and (31)P NMR spectroscopy and by ESI-mass experiments. The NMR studies allowed to establish that the intercalation between the base pairs of the duplex leads to very stable complexes and at the same time to exclude the formation of covalent bonds. Melting experiments monitored by NMR, allowed to observe with high accuracy the behaviour of the imine protons with temperature, and the results showed that the re-annealing occurs after melting.
Mazzini S1, Scaglioni L, Mondelli R, Caruso M, Sirtori FR. Bioorg Med Chem. 2012 Dec 15;20(24):6979-88. doi: 10.1016/j.bmc.2012.10.033. Epub 2012 Nov 3.
The antitumor anthracycline nemorubicin is converted by human liver microsomes to a major metabolite, PNU-159682 (PNU), which was found to be much more potent than its parent drug toward cultured tumor cells and in vivo tumor models. The mechanism of action of nemorubicin appears different from other anthracyclines and until now is the object of studies. In fact PNU is deemed to play a dominant, but still unclear, role in the in vivo antitumor activity of nemorubicin. The interaction of PNU with the oligonucleotides d(CGTACG)(2), d(CGATCG)(2) and d(CGCGCG)(2) was studied with a combined use of (1)H and (31)P NMR spectroscopy and by ESI-mass experiments. The NMR studies allowed to establish that the intercalation between the base pairs of the duplex leads to very stable complexes and at the same time to exclude the formation of covalent bonds. Melting experiments monitored by NMR, allowed to observe with high accuracy the behaviour of the imine protons with temperature, and the results showed that the re-annealing occurs after melting.
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