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144510-96-3

中文名稱 匹杉瓊
英文名稱 Pixantrone
CAS 144510-96-3
分子式 C17H19N5O2
分子量 325.37
MOL 文件 144510-96-3.mol
更新日期 2024/06/03 14:41:43
144510-96-3 結(jié)構(gòu)式 144510-96-3 結(jié)構(gòu)式

基本信息

中文別名
匹杉瓊
匹克生瓊
馬來酸匹杉瓊
匹杉瓊二馬來酸鹽
拓?fù)洚悩?gòu)酶Ⅱ抑制劑
PIXANTRONEBBR 2778匹杉瓊
6,9-二[(2-氨乙基)氨基]苯并[G]異喹啉-5,10-二酮
英文別名
CS-1359
pixantrone
Pixantrone Dimaleate
Pixantrone, BBR 2778
BBR-2778
BBR2778
BBR 2778
Pixantrone diformate salt
6,9-Bis[(2-aminoethyl)amino]benz[g]isoquinoline-5,10-dione
6,9-bis((2-aminoethyl)amino)benzo(g)isoquinoline-5,10-dione
Benz[g]isoquinoline-5,10-dione, 6,9-bis[(2-aminoethyl)amino]-
所屬類別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

熔點(diǎn)>173°C (dec.)
密度1.405
儲(chǔ)存條件Refrigerator
溶解度可溶于DMSO(少許)、甲醇(少許)
形態(tài)固體
顏色深藍(lán)色至深藍(lán)色

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335

常見問題列表

生物活性
Pixantrone 是一種拓?fù)洚悩?gòu)酶 II (topoisomerase II) 的抑制劑和 DNA 嵌入劑,具有抗腫瘤活性。
靶點(diǎn)

Topoisomerase II

體外研究

Pixantrone is a topoisomerase II inhibitor. Pixantrone induces cell death in multiple cancer cell lines independent of cell cycle perturbation, with IC 50 s of 37.3 nM, 126 nM and 136 nM for T47D, MCF-10A and OVCAR5 cells, respectively. Pixantrone induces DNA damage at high concentrations (500 nM) but not at concentrations (100 nM) sufficient to kill PANC1 cells. Pixantrone (25 or 100 nM) induces severe chromosomal aberrations and mitotic catastrophe in PANC1 cells. Pixantrone (100 nM) may disrupt chromosome segregation because of generating merotelic kinetochore attachments that cause chromosome non-disjunction. Pixantrone potently inhibits growth of human Leukemia K562 cells, etoposide-resistant K/VP.5 cells, MDCK and ABCB1-transfected MDCK/MDR cells, with IC 50 s of 0.10 μM, 0.56 μM, 0.058 μM and 4.5 μM, respectively. Pixantrone (0.01-0.2 μM) leads to a concentration-dependent formation of linear DNA through acting on topoisomerase IIα. Pixantrone produces semiquinone free radicals in an enzymatic reducing system, although not in a cellular system, most likely due to low cellular uptake. Pixantrone (0.01-10 μM) shows potent inhibitory activities against rat 97-116 peptide-specific T cell proliferation.

體內(nèi)研究

Pixantrone (27 mg/kg) does not worsen pre-existing moderate degenerative cardiomyopathy in doxorubicin-pretreated mice, by i.v. one dose every 7 days repeated thrice (q7d × 3). Pixantrone (27 mg/kg) causes minimal cardiotoxic in mice following repeated treatment cycles. Moreover, Pixantrone results in less mortality than mitoxantrone in doxorubicin-pretreated mice. Pixantrone (16.25 mg/kg i.v, q7d × 3) modulates Lymph node cells (LNC) responses, and affacts T cell subpopulations in TAChR-immunized Lewis rats. Pixantrone also shows preventive and therapeutic effect in experimental autoimmune myasthenia gravis (EAMG) rats.

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