吡柔比星作用機制 - Medchemexpress - MCE中國

1、Product Data SheetPirarubicinCat. No.: HY-13725CAS No.: 72496-41-4分式: CHNO分量: 627.64作靶點: Topoisomerase; Autophagy; Bacterial作通路: Cell Cycle/DNA Damage; Autophagy; Anti-infection儲存式: 4C, protect from light* 該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)現(xiàn)配，即刻使。溶解性數(shù)據(jù)體外實驗 DMSO : 50 mg/mL (79.66 mM; Need ultrasonic)SolventMass1 mg 5

2、mg 10 mgConcentration制備儲備液1 mM 1.5933 mL 7.9664 mL 15.9327 mL5 mM 0.3187 mL 1.5933 mL 3.1865 mL10 mM 0.1593 mL 0.7966 mL 1.5933 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)現(xiàn)配，即刻使.體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天 使；

3、 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可 以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (3.98 mM); Clear solution此案可獲得 2.5 mg/mL (3.98 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 4

4、50 L 理鹽定容 1 mL。BIOLOGICAL ACTIVITY物活性 Pirarubicin療。種蒽環(huán)類抗素，為拓撲異構(gòu)酶 II (topoisomerase II) 的抑制劑，可于各種癌癥尤其是固體腫瘤的治Page 1 of 2 www.MedChemEIC & Target Topoisomerase II體外研究 Pirarubicin is a topoisomerase II inhibitor1. Pirarubicin shows inhibitory activities against M5076 and Ehrlich cells,with IC50s of 0.36

5、6 and 0.078 M, respectively. The cytotoxicity of Pirarubicin toward M5076 cells is lower than towardEhrlich cells, and this is due to the much lower expression of topoisomerase II in M5076 cells than in Ehrlich cells2.Pirarubicin (2.5, 5, 10 g/mL) significantly induces autophagy in a dose dependent

6、manner in bladder cancer (T24, EJ,5637, J82 and UM-UC-3) cells. Furthmore, Pirarubicin (5 g/mL) induces apoptosis through inhibition ofmTOR/p70S6K/4E-BP1 in bladder cancer cells, and this effect is enhanced by inhibition of autophagy3.體內(nèi)研究 Pirarubicin (18 mg/kg, i.v.) significantly elevates serum le

7、vel of BNP, CK-MB, CTnT, LDH, and MDA compared withthose in the control group in acute cardiac toxicity rats. Pirarubicin also lowers heart rate, and depresses R-wavevoltage, and prolongation of QT intervals in the acute cardiac toxicity model4.PROTOCOLCell Assay 3 MTS is used to analyze cell surviv

8、al. Briefly, cells are plated in 96-well plates in triplicate at 2 103 cells per well andcultured in growth medium. Then cells are treated with pirarubicin at different concentrations (2.5 g/mL, 5 g/mL,10 g/mL) for 24 h. MTS reagent (5 mg/mL) is added and incubated at 37C for 4 h. The absorbance is

9、monitored at490 nm using a microplate reader3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal An acute cardiac toxicity model is established by a single dose of 18 mg/kg pirarubicin through the caudal veinAdministration 4 injection. Thirty-six ra

10、ts are randomized equally to six groups: normal control, cardiac injury (THP) model,dexrazoxane (180 mg/kg), low-dose rutin (25 mg/kg), middle-dose rutin (50 mg/kg), and high-dose rutin (100mg/kg). Rats in the rutin-treated group are administered different doses of rutin and CMC-Na for 7 days by gav

11、ageand a single dose of 18 mg/kg pirarubicin through caudal vein injection. Rats in the dexrazoxane-treated groupreceive sodium carboxymethylcellulose (CMC-Na) by gavage for six days. 40 mg/kg dexrazoxane is then administeredto rats by intraperitoneal injection and 18 mg/kg pirarubicin is administer

12、ed by caudal vein injection on day 7. Rats inthe THP model group receive CMC-Na by gavage for seven days, followed by pirarubicin 18 mg/kg through thecaudal vein injection on day 7. Rats in the normal control group receive CMC-Na by gavage for seven days, followedby saline through caudal vein inject

13、ion on day 74.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 J Mol Med (Berl). 2019 Aug;97(8):1183-1193.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Takigawa N, et al. Cytotoxic effect of topoisomerase II

14、 inhibitors against adriamycin- and etoposide-resistant small cell lung cancer sublines. Gan ToKagaku Ryoho. 1993 May;20(7):929-35.2. Nagai K, et al. Relationships between the in vitro cytotoxicity and transport characteristics of pirarubicin and doxorubicin in M5076 ovarian sarcoma cells,and compar

15、ison with those in Ehrlich ascites carcinoma cells. Cancer Chemother Pharmacol. 2002 Mar;49(3):244-50. Epub 2002 Jan 8.3. Li K, et al. Pirarubicin induces an autophagic cytoprotective response through suppression of the mammalian target of rapamycin signaling pathway inPage 2 of 3 www.MedChemEhuman bladder cancer cells. Biochem Biophys Res Commun. 2015 May 1;460(2):380-5.4. Wang YD, et al. Cardioprotective effects of rutin in rats exposed to pirarubicin toxicity. J Asian Nat Prod Res. 201