Mitoxantrone-mitozantrone-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMitoxantroneCat. No.: HY-13502CAS No.: 65271-80-9Synonyms: mitozantrone分式: CHNO分量: 444.48作靶點(diǎn): Topoisomerase; PKC作通路: Cell Cycle/DNA Damage; Epigenetics; TGF-beta/Smad儲(chǔ)存式: -20C, protect from light* In solvent : -80C, 6 months; -2

2、0C, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 25 mg/mL (56.25 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.2498 mL 11.2491 mL 22.4982 mL5 mM 0.4500 mL 2.2498 mL 4.4996 mL10 mM 0.2250 mL 1.1249 mL 2.2498 mL請(qǐng)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(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適

3、當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.62 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.62 mM); Clear so

4、lutionBIOLOGICAL ACTIVITY1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 Mitoxantrone拓?fù)洚悩?gòu)酶II (topoisomerase II)的抑制劑；也可抑制蛋激酶C (PKC)， IC50值為8.5 M。IC50 & Target PKC Topoisomerase II8.5 M (IC50)體外研究 Mitoxantrone inhibits PKC in a competitive manner with respect to histone H1, and its Ki value is 6.

5、3 M andin a non-competitive manner with respect to phosphatidylserine and ATP 1. Treatment of B-CLL cells for 48h with mitoxantrone (0.5 g/mL) induces a decrease in cell viability. Mitoxantrone induces DNA fragmentationand the proteolytic cleavage of poly(ADP-ribose) polymerase (PARP), demonstrating

6、 that the cytotoxic effectof mitoxantrone is due to induction of apoptosis 2. Mitoxantrone shows cytotoxicity to human breastcarcinoma cell lines MDA-MB-231 and MCF-7 with IC50 values of 18 and 196 nM, respectively 3.體內(nèi)研究 Mitoxantrone given IP at the optimal dose (1.6 mg/kg/day; as a free base) prod

7、uces a statistically significantnumber of 60-day survivors (curative effect) in mice with IP implanted L1210 leukemia. In SC implantedLewis lung carcinoma, mitoxantrone and ADM administered IV also shows effective antitumor activities andproduces a 60% and a 45% ILS, respectively. 4.PROTOCOLCell Ass

8、ay 3 The human breast carcinoma cell lines MDA-MB-231 and MCF-7 are seeded in standard 96-well plates. Oneday after seeding, the culture medium is changed and replaced by medium containing different concentrationof Mitoxantrone (10-5 to 5 M) with or without DHA (30 M) during 7 days. Viability of cel

9、ls are measured asa whole by the tetrazolium salt assay 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: Mitoxantrone is tested for antitumor activity against experimental tumors in mice and the results areAdministration 4 compared with th

10、ose of seven antitumor antibiotics. The drugs are given IP or IV, in general on days 1, 5,and 9 following tumor inoculation. Mitoxantrone is given IP at the optimal dose (1.6 mg/kg/day; as a freebase) 4.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使

11、本產(chǎn)品發(fā)表的科研獻(xiàn) J Mol Med (Berl). 2019 Jun 14.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Takeuchi N, et al. Inhibitory effect of mitoxantrone on activity of protein kinase C and growth of HL60 cells. J Biochem. 1992Dec;112(6):762-7.2. Bellosillo B, et al. Mitoxantrone, a topoiso

12、merase II inhibitor, induces apoptosis of B-chronic lymphocytic leukaemia cells. Br J Haematol.1998 Jan;100(1):142-6.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. Vibet S, et al. Differential subcellular distribution of mitoxantrone in relation to chemosensitization in two human breast cancer cell lines.Drug Metab Dispos. 2007 May;35(5):822-8.4. Fujimoto S, et al. Antitumor activity of mitoxantrone against murine experimental tumors: comparative analysis against various antitumorantibiotics. Cancer Chemother Pharmacol. 1982;8(2):157-62.McePdfHei