中文名 | 盐酸胺苯吖啶 |
英文名 | Amsacrine hydrochloride |
别名 | 胺苯丫啶 安沙克林 安吖啶盐酸盐 盐酸胺苯吖啶 N-[4-(9-吖啶基氨基)-3-甲氧基苯基]甲基磺酰胺 N-[4-(9-吖啶氨基)-3-甲氧苯基]甲基磺酰胺盐酸盐 盐酸胺苯吖啶,安吖啶,胺苯吖啶,N-[4-(9-吖啶基氨基)-3-甲氧基苯基]甲基磺酰胺 |
英文别名 | M-AMSA, HCL M-AMSA HYDROCHLORIDE Amsacrine hydrochloride Methanesulfon-m-anisidide 4'-(9-acridinylamino)- Methanesulfone-m-anisidine-4'-[(9-acridinyl)amino] hydrochloride Methansulfon-m-aniside, 4'-(9-acridinylamino)-, monohydrochloride 4-[9-ACRIDINYLAMINO]-N-[METHANE-SULFONYL]-M-ANISIDINE HYDROCHLORIDE m-AMSA, 4-(9-Acridinylamino)-N-(methanesulfonyl)-m-anisidine hydrochloride Methanesulfonamide, N-4-(9-acridinylamino)-3-methoxyphenyl-, monohydrochloride |
CAS | 54301-15-4 |
EINECS | 637-255-8 |
化学式 | C21H20ClN3O3S |
分子量 | 429.92 |
熔点 | 197-199°C(lit.) |
溶解度 | DMSO: 10mg/ml,加热和超声处理 |
存储条件 | Refrigerator |
外观 | 粉末 |
颜色 | red to brown |
MDL号 | MFCD07799963 |
体外研究 | Amsacrine (mAMSA) blocks HERG currents in HEK 293 cells and Xenopus oocytes in a concentration-dependent manner, with IC 50 values of 209.4 nM and 2.0 μM, respectively. Amsacrine (mAMSA) causes a negative shift in the voltage dependence of both activation (−7.6 mV) and inactivation (−7.6 mV). HERG current block by Amsacrine (mAMSA) is not frequency dependent. In vitro studies of normal human lymphocytes with various concentrations of Amsacrine (mAMSA), show both increased levels of chromosomal aberrations, ranging from 8% to 100%, and increase SCEs, ranging from 1.5 times the normal at the lowest concentration studied (0.005 μg/mL) to 12 times the normal (0.25 μg/mL). Amsacrine (mAMSA)-induced apoptosis of U937 cells is characterized by caspase-9 and caspase-3 activation, increased intracellular Ca 2+ concentration, mitochondrial depolarization, and MCL1 down-regulation. Amsacrine induces MCL1 down-regulation by decreasing its stability. Further, amsacrine-treated U937 cells show AKT degradation and Ca 2+ -mediated ERK inactivation. |
体内研究 | In animals treated with different doses of amsacrine (0.5-12 mg/kg), the frequencies of micronucleated polychromatic erythrocytes increase significantly after treatment with 9 and 12 mg/kg. Furthermore, the present study demonstrates for the first time that Amsacrine (mAMSA) has high incidences of clastogenicity and low incidences of aneugenicity whereas nocodazole has high incidences of aneugenicity and low incidences of clastogenicity during mitotic phases in vivo. |
危险品标志 | T - 有毒物品![]() |
风险术语 | R25 - 吞食有毒。 R36/37/38 - 刺激眼睛、呼吸系统和皮肤。 |
安全术语 | S26 - 不慎与眼睛接触后,请立即用大量清水冲洗并征求医生意见。 S45 - 若发生事故或感不适,立即就医(可能的话,出示其标签)。 |
危险品运输编号 | UN 2811 6.1/PG 3 |
WGK Germany | 3 |
RTECS | PB1081000 |
Hazard Class | 6.1(b) |
Packing Group | III |
下游产品 | 安吖啶 |
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