宾达氮芥

中文名称:

宾达氮芥

中文同义词:

宾达氮芥;苯达莫司汀;4-[5-[双(2-氯乙基)氨基]-1-甲基苯并咪唑-2-基]丁酸;盐酸苯达莫司汀/4-[5-[双(2-氯乙基)氨基]-1-甲基苯并咪唑-2-基]丁酸

英文名称:

Bendamustine

英文同义词:

5-(Bis(2-chloroethyl)amino)-1-methyl-2-benzimidazolebutyric acid;5-[Bis(2-chloroethyl)amino]-1-methyl-1H-benzimidazole-2-butanoic acid;Bendamustine;-1-methyl-1H-benzo[d]imidazol-2-yl);4-(5-(Bis(2-chloroethyl);4-[5-[bis(2-chloroethyl)amino]-1-methylbenzimidazol-2-yl]butanoic acid;4-(5-(bis(2-chloroethyl)aMino)-1-Methyl-1H-benzo[d]iMidazol-2-yl)butanoic acid;1H-BenziMidazole-2-butanoicacid, 5-[bis(2-chloroethyl)aMino]-1-Methyl-

CAS号:

16506-27-7

分子式:

C16H21Cl2N3O2

分子量:

358.26

EINECS号:

相关类别:

杂环类

Mol文件:

16506-27-7.mol

沸点 

585.2±50.0 °C(Predicted)

密度 

1.31±0.1 g/cm3(Predicted)

酸度系数(pKa)

4.50±0.10(Predicted)

生物活性

Bendamustine (SDX105)是一种氮芥药物，用于治疗慢性淋巴细胞白血病、多发性骨髓瘤和非霍奇金淋巴瘤。

靶点

DNA Alkylator/Crosslinker

体外研究

Bendamustine is a DNA cross-linking agent that causes DNA breaks, with alkylating and antimetabolite properties. Bendamustine uniquely regulates apoptosis pathways and DNA repair pathways in non-Hodgkins lymphoma cells. Bendamustine (50 μM) induces p21 (Cip1/Waf1) and NOXA genes, and increases the expression of p53 in SU-DHL-1 cells. Bendamustine (25 μM) blocks mitotic checkpoints and cuases mitotic catastrophe. Bendamustine reduces the viability of multiple myeloma (MM) cell lines, such as RPMI-8226 and 8226-LR5 cells, with IC 25 s of 101.8 μM and 585.5 μM after 24 h incubation, and 51.7 and 374.3 μM after 48 h incubation, respectively. Bendamustine induces a specific caspase-dependent MM cell death and inhibits the spindle-assembly checkpoint.

体内研究

Bendamustine (25 mg/kg, i.v.) shows potent inhibition on the growth of tumor cells by 91%, 99% and 95% for DoHH-2, Granta 519 and RAMOS models, respectively. Moreover, the antitumor effect of Bendamustine is enhanced by rituximab in DoHH-2 and RAMOS models, but not in Granta 519 model.