中文名 | 宾达氮芥 |
英文名 | Bendamustine |
别名 | 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 4-(5-(双(2-氯乙基)氨基)-1-甲基-1H-苯并[D]咪唑-2-基)丁酸 |
英文别名 | Bendamustine 4-(5-(Bis(2-chloroethyl) -1-methyl-1H-benzo[d]imidazol-2-yl) 5-(Bis(2-chloroethyl)amino)-1-methyl-2-benzimidazolebutyric acid 5-[Bis(2-chloroethyl)amino]-1-methyl-1H-benzimidazole-2-butanoic acid 1H-BenziMidazole-2-butanoicacid, 5-[bis(2-chloroethyl)aMino]-1-Methyl- 4-[5-[bis(2-chloroethyl)amino]-1-methylbenzimidazol-2-yl]butanoic acid 4-{5-[Bis(2-chloroethyl)amino]-1-methyl-1H-benzimidazol-2-yl}butanoic acid 4-(5-(bis(2-chloroethyl)aMino)-1-Methyl-1H-benzo[d]iMidazol-2-yl)butanoic acid |
CAS | 16506-27-7 |
化学式 | C16H21Cl2N3O2 |
分子量 | 358.26 |
InChI | InChI=1/C16H21Cl2N3O2/c1-20-14-6-5-12(21(9-7-17)10-8-18)11-13(14)19-15(20)3-2-4-16(22)23/h5-6,11H,2-4,7-10H2,1H3,(H,22,23) |
密度 | 1.31±0.1 g/cm3(Predicted) |
沸点 | 585.2±50.0 °C(Predicted) |
闪点 | 307.7°C |
蒸汽压 | 1.55E-14mmHg at 25°C |
折射率 | 1.599 |
酸度系数 | 4.50±0.10(Predicted) |
存储条件 | 2-8°C |
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-Hodgkin's 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. |
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