帕利伐米

概述生物活性体外研究体内研究帕利伐米试剂级价格

帕利伐米

CAS号:31645-39-3
英文名:Palifosfamide
中文名:帕利伐米
CBNumber:CB11011411
分子式:C4H11Cl2N2O2P
分子量:221.02
MOL File:31645-39-3.mol

帕利伐米化学性质

熔点 :106-107 ºC
沸点 :341.5±52.0 °C(Predicted)
密度 :1.411
储存条件 :Store at -20°C, protect from light, stored under nitrogen
溶解度 :≥22.1 mg/mL in DMSO; insoluble in EtOH; ≥19.4 mg/mL in H2O with gentle warming and ultrasonic
形态 :Powder
酸度系数(pKa) :0.79±0.50(Predicted)
InChI :InChI=1S/C4H11Cl2N2O2P/c5-1-3-7-11(9,10)8-4-2-6/h1-4H2,(H3,7,8,9,10)
InChIKey :BKCJZNIZRWYHBN-UHFFFAOYSA-N
SMILES :P(NCCCl)(NCCCl)(O)=O
CAS 数据库 :31645-39-3

帕利伐米性质、用途与生产工艺

概述帕利伐米（IPM）是环磷酰胺（CPA）的常见代谢产物。帕利伐米被认为是CPA表现出的至少一部分抗肿瘤活性的原因。直接使用帕利伐米作为抗癌剂的努力未获成功，部分原因是该化合物的不稳定性。已经合成了帕利伐米并且已经对该化合物进行了初步的生物学评估，但遗憾的是帕利伐米太不稳定而不能被分离并用于人类治疗。
生物活性 Palifosfamide (ZIO-201, Isophosphamide mustard)是新型的DNA烷化剂，是异环磷酰胺（ifosfamide）的活性代谢产物，具有抗肿瘤活性。
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.