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78186-34-2

中文名稱 比生群
英文名稱 Bisantrene
CAS 78186-34-2
分子式 C22H22N8
分子量 398.46
MOL 文件 78186-34-2.mol
更新日期 2024/07/24 18:26:20
78186-34-2 結(jié)構(gòu)式 78186-34-2 結(jié)構(gòu)式

基本信息

中文別名
比生群
必桑那
必???BR>比索布啉
咪蒽二腙
比生群, >96%
9,10-蒽二甲醛雙(4,5-二氫-1H-咪唑-2-基)腙
9,10-蒽二醛雙[(4,5-二氫-1H-咪唑-2-基)腙]
Bisantrene(含有少量DMSO) (Free base)
BISANTRENE(含有少量DMSO) (FREE BASE)
英文別名
ADAH
CS-2227
Zantrene
CL-216942
BISANTRENE
NSC-337766
Orange Crush
BISANTRENE HCL
Bisantrene, >96%
Bisantrene USP/EP/BP
所屬類別
藥物: 抗腫瘤藥: 其它抗腫瘤藥物

物理化學性質(zhì)

外觀性狀二鹽酸比生群(Bisantrene Dihydrochlofide):C22H22N8?2HCl。[71439-68-4]。從乙醇得橙色結(jié)晶性固體。其半水合物熔點288~289℃(分解)。UV最大吸收(水):260,415nm(ε72700,16300)
沸點646.3±65.0 °C(Predicted)
密度1.41±0.1 g/cm3(Predicted)
儲存條件room temp
溶解度去離子水中的溶解度:8mg/mL
酸度系數(shù)(pKa)9.78±0.10(Predicted)
形態(tài)固體
顏色Orange to red
InChIKeyNJSMWLQOCQIOPE-OCHFTUDZSA-N
SMILESC1(/C=N/NC2=NCCN2)=C2C=CC=CC2=C(/C=N/NC2=NCCN2)C2C=CC=CC1=2

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictogramsGHS hazard pictograms
GHS07,GHS09
警示詞警告
危險性描述H302-H400
危險品標志Xn,N
危險類別碼22-50/53
安全說明60-61
危險品運輸編號UN 2811 6.1 / PGIII
WGK Germany3

應用領域

用途1
蒽環(huán)類細胞生長抑制劑,用于抗腫瘤。對惡性淋巴瘤、黑色素瘤、急性白血病、卵巢癌和腎癌有效。

制備方法

方法1
9,10-蒽二醛和2-肼基-2-咪唑啉二鹽酸鹽反應,得二鹽酸比生群。

常見問題列表

生物活性
Bisantrene 是一種高效的抗腫瘤藥物,靶向作用于真核生物的II型拓撲異構(gòu)酶 (II topoisomerases)。
靶點

Topoisomerase II

體內(nèi)研究

Bisantrene shows an outstanding ability to form a complex with DNA. Bisantrene exhibits the most effective binding (even neglecting electrostatic contacts), followed by the 9-substituted compounds and finally by 1-IHA. Bisantrene congeners retained a remarkable capacity for binding to the single-stranded structure. In comparison with the K i values found for double-stranded DNA, 9-IHA shows a 2-fold increase, 1-IHA maintains the same values, and aza-9-IHA exhibits a modest reduction. On the other hand, Bisantrene, although undergoing a 6-fold reduction in K i , still exhibits an affinity constant of the order of 10 6 M -1 . Bisantrene promots DNase I cleavage at oligopurine-oligopyrimidine tracts; conversely, it slightly reduces the cleavage activity at alternating purine-pyrimidine sequences. Bisantrene is an active new drug in the treatment of metastatic breast cancer. Bisantrene is an inhibitor of [ 3 H]uridine incorporation into RNA and [ 3 H]thymidine incorporation into DNA.

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