中文名 | 帕利伐米 |
英文名 | Palifosfamide |
别名 | 帕利伐米 N,N'-双(2-氯乙基)二氨基膦酸 |
英文别名 | Ipam palifosfamide Palifosfamide Ifosforamide mustard Isophosphamide mustard N,N'-BIS(2-CHLOROETHYL)PHOSPHORODIAMIDATE N,N'-Di-(2-chloroethyl)phosphorodiamidic acid N,N'-Bis(2-chloroethyl)phosphorodiamidic acid |
CAS | 31645-39-3 |
化学式 | C4H11Cl2N2O2P |
分子量 | 221.02 |
InChI | InChI=1/C4H11Cl2N2O2P/c5-1-3-7-11(9,10)8-4-2-6/h1-4H2,(H3,7,8,9,10) |
密度 | 1.411 |
熔点 | 106-107 ºC |
沸点 | 341.5±52.0 °C(Predicted) |
闪点 | 160.4°C |
蒸汽压 | 1.45E-05mmHg at 25°C |
折射率 | 1.497 |
酸度系数 | 0.79±0.50(Predicted) |
存储条件 | -20℃ |
体外研究 | Palifosfamide lysine (ZIO-201) is a stable form of palifosfamide. Palifosfamide lysine has broad activity in sarcoma lines in vitro . The IC 50 ranges from 2.25 ro 6.75 μM for most cell lines except OS222 (IC 50 =31.5 μM). |
体内研究 | Tumor growth inhibition is seen in both OS31 and OS33 xenografts and the RMS xenograft resulting in a significant difference in event-free survival between the control and the treated groups. Differential gene expression of ALDH3A1 but not ALDH1A1 is noted in the OS31 xenograft. Stabilized palifosfamide administered to mice suppresses MX-1 tumor growth by greater than 80% with 17% complete antitumor responses. Oral bioavailability in rats is 48-73% of parenteral administration, and antitumor activity in mice is equivalent by both routes. Treatment with palifosfamide-tris combined with docetaxelor doxorubicin at optimal regimens results in complete tumor regression in 62-75% of mice. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 4.524 ml | 22.622 ml | 45.245 ml |
5 mM | 0.905 ml | 4.524 ml | 9.049 ml |
10 mM | 0.452 ml | 2.262 ml | 4.524 ml |
5 mM | 0.09 ml | 0.452 ml | 0.905 ml |
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