米托蒽醌

生物活性靶点体外研究体内研究米托蒽醌试剂级价格

米托蒽醌

CAS号:65271-80-9
英文名:Mitoxantrone
中文名:米托蒽醌
CBNumber:CB1246423
分子式:C22H28N4O6
分子量:444.48
MOL File:65271-80-9.mol

米托蒽醌化学性质

熔点 :170-1740C
沸点 :554.47°C (rough estimate)
密度 :1.3049 (rough estimate)
折射率 :1.6500 (estimate)
储存条件 :Keep in dark place,Sealed in dry,2-8°C
溶解度 :DMSO (Slightly), Methanol (Sparingly), Water (Slightly)
酸度系数(pKa) :pKa 5.99 (Uncertain);8.13 (Uncertain)
形态 :Solid
颜色 :Dark Blue to Black
InChI :InChI=1S/C22H28N4O6/c27-11-9-23-5-7-25-13-1-2-14(26-8-6-24-10-12-28)18-17(13)21(31)19-15(29)3-4-16(30)20(19)22(18)32/h1-4,23-30H,5-12H2
InChIKey :KKZJGLLVHKMTCM-UHFFFAOYSA-N
SMILES :C1(O)=C2C(C(=O)C3=C(C2=O)C(NCCNCCO)=CC=C3NCCNCCO)=C(O)C=C1
CAS 数据库 :65271-80-9(CAS DataBase Reference)
(IARC)致癌物分类 :2B (Vol. 76) 2000

安全信息

危险品标志 :T,T+
危险类别码 :46-61-26/27/28
安全说明 :53-36/37/39-45-22
WGK Germany :3
RTECS号 :CB5748500
海关编码 :2922.50.2500

米托蒽醌化学药品说明书

米托蒽醌|药物应用信息

米托蒽醌性质、用途与生产工艺

生物活性 Mitoxantrone是拓扑异构酶II (topoisomerase II)的抑制剂；也可抑制蛋白激酶C (PKC)， IC50值为8.5 μM。
靶点

PKC

8.5 μM (IC ₅₀ )

Topoisomerase II
体外研究

Mitoxantrone inhibits PKC in a competitive manner with respect to histone H1, and its K _i value is 6.3 μM and in a non-competitive manner with respect to phosphatidylserine and ATP. Treatment of B-CLL cells for 48 h with mitoxantrone (0.5 μg/mL) induces a decrease in cell viability. Mitoxantrone induces DNA fragmentation and the proteolytic cleavage of poly(ADP-ribose) polymerase (PARP), demonstrating that the cytotoxic effect of mitoxantrone is due to induction of apoptosis. Mitoxantrone shows cytotoxicity to human breast carcinoma cell lines MDA-MB-231 and MCF-7 with IC ₅₀ values of 18 and 196 nM, respectively.
体内研究

Mitoxantrone given IP at the optimal dose (1.6 mg/kg/day; as a free base) produces a statistically significant number of 60-day survivors (curative effect) in mice with IP implanted L1210 leukemia. In SC implanted Lewis lung carcinoma, mitoxantrone and ADM administered IV also shows effective antitumor activities and produces a 60% and a 45% ILS, respectively..
化学性质蓝黑色结晶。熔点203-205℃。略溶于水，微溶于乙醇，不溶于氯仿和丙酮。无臭，易吸潮
用途蒽环类抗癌药，抗癌活性与阿霉素相似或略高，明显高于环磷酰胺、阿糖胞苷、甲氨喋呤、氟脲嘧啶、长春新碱等常用的抗癌药。临床用于乳腺癌有突出的疗效。