伐司扑达
中文名称 | 伐司扑达 |
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中文同义词 | 伐司扑达;戊司泊达;P-糖蛋白抑制剂(VALSPODAR);伐司朴达;(3S,6S,9S,12R,15S,18S,21S,24S,30S,33S)-6,9,18,24-四异丁基-3,21,30-三异丙基-1,4,7,10,12,15,19,25,28-九甲基-33-((R,E)-2-甲基己-4-烯酰基)-1,4,7,10,13,16,19,22,25,28,31-十一氮杂环三十三烷-2,5,8,11,14,17,20,23,26,29,32-十一酮 |
英文名称 | Valspodar |
英文同义词 | Valspodar;3'-Keto-bmt(1)-Val(2)-cyclosporin a;Cyclosporin A, 6-((R-(E))-6,7-didehydro-N,4-dimethyl-3-oxo-L-2-aminooctanoic acid)-7-L-valine-;Sdz psc 833;Sdz-psc-833;Cyclo[[(2S,4R,6E)-4-methyl-2-(methylamino)-3-oxo-6-octenoyl]-L-valyl-N-methylglycyl-N-methyl-L-leucyl-L-valyl-N-methyl-L-leucyl-L-alanyl-D-alanyl-N-methyl-L-leucyl-N-methyl-L-leucyl-N-methyl-L-valyl];6-[(2S,4R,6E)-4-methyl-2-(methylamino)-3-oxo-6-octenoicacid]-7-L-valine-cyclosporinA;Valspodar(PSC-833,AMdray) |
CAS号 | 121584-18-7 |
分子式 | C63H111N11O12 |
分子量 | 1214.62 |
EINECS号 | 1312995-182-4 |
相关类别 | 抑制剂;细胞生物学试剂;Intermediates & Fine Chemicals;Peptides;Pharmaceuticals |
Mol文件 | 121584-18-7.mol |
结构式 |
伐司扑达 性质
熔点 | 143-145°C |
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比旋光度 | D20 -255.1° (c = 0.5 in CHCl3) |
沸点 | 1290.1±65.0 °C(Predicted) |
密度 | 1.015±0.06 g/cm3(Predicted) |
储存条件 | -20°C |
溶解度 | 可溶于氯仿(少许)、甲醇(少许) |
酸度系数(pKa) | 12.45±0.70(Predicted) |
形态 | 粉末 |
颜色 | 白色至米色 |
InChIKey | YJDYDFNKCBANTM-QCWCSKBGSA-N |
Valspodar (PSC 833) has no cytotoxicity effects at up to the concentration of 0.75 μg/mL. Valspodar (0.25, 0.5 and 0.75 μg/mL) and DOX-L are added to the DOX resistant cells, and cell kill efficacy of MDR cell type increases significantly when valspodar is administered alongside DOX-L. Valspodar (0.5 and 0.75 μg/mL), in combination with all concentrations of DOX, are most toxic and kill more than 70% of the resistant cells. Pretreatment with PSC833 decreases the IC 50 value of NSC 279836 in MDA-MB-435mdr cells to 0.4±0.02 μM in MDR cells and almost completely reverses the resistance of MDR cells to NSC 279836.
valspodar (10 mg/kg, o.p.) exhibits minimal blood-cell partitioning as reflected in its low mean blood-to-plasma ratio of approximately 0.52. Valspodar displays properties of slow clearance and a large volume of distribution. Valspodar shows properties of low hepatic extraction and wide distribution, similar to that of its structural analogue CsA. Preadministration of PSC833 to mice increases NSC 279836 fluorescent intensity in MDR tumor to 94% of that in the wild-type tumors.
安全信息
WGK Germany | 3 |
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更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-17384 | 伐司扑达 Valspodar | 121584-18-7 | 1mg | 3500元 |
2023/03/20 | HY-17384 | 伐司扑达 Valspodar | 121584-18-7 | 5mg | 11200元 |