Mitoxantrone-mitozantrone-DataSheet-生命科学试剂-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作靶点: Topoisomerase; PKC作通路: Cell Cycle/DNA Damage; Epigenetics; TGF-beta/Smad储存式: -20C, protect from light* In solvent : -80C, 6 months; -2

2、0C, 1 month (protect fromlight)溶解性数据体外实验 DMSO : 25 mg/mL (56.25 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液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，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适

3、当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.62 mM); Clear solution2. 请依序添加每种溶剂： 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 您边的抑制剂师www.MedChemE物活性 Mitoxantrone拓扑异构酶II (topoisomerase II)的抑制剂；也可抑制蛋激酶C (PKC)， IC50值为8.5 M。IC50 & Target PKC Topoisomerase II8.5 M (IC50)体外研究 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.体内研究 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.户使

11、本产品发表的科研献 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 您边的抑制剂师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