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Palifosfamide

Palifosfamide

产品编号 T4350   CAS 31645-39-3
别名: ZIO-201, Isophosphamide mustard, 帕利伐米, Isophosphoramide mustard

Palifosfamide (Isophosphamide mustard) 是一种新 DNA 烷化剂,是异环磷酰胺的活性代谢物,。它在体外肉瘤细胞系中具有广泛的活性,具有抗癌活性。

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Palifosfamide Chemical Structure
Palifosfamide, CAS 31645-39-3
规格 价格/CNY 货期 数量
1 mg ¥ 561 现货
2 mg ¥ 828 现货
5 mg ¥ 1,390 现货
10 mg ¥ 2,320 现货
25 mg ¥ 3,950 现货
50 mg ¥ 5,630 现货
100 mg ¥ 7,880 现货
1 mL * 10 mM (in DMSO) ¥ 1,550 现货
其他形式的 Palifosfamide:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
产品目录号及名称: Palifosfamide (T4350)
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纯度: 97%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Palifosfamide (Isophosphamide mustard) lysine (ZIO-201) is a stable form of palifosfamide. Palifosfamide lysine has broad activity in sarcoma lines in vitro. The IC50 ranges from 2.25 to 6.75 μM for most cell lines except OS222 (IC50=31.5 μM).
靶点活性 OS222:31.5 μM
体外活性 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.
细胞实验 Palifosfamide is dissolved in phosphate buffered saline (PBS). Cells are plated in 96-well microtiter plates with approximately 500 cells per well in 100 μL of media. After 24 h of incubation at 37°C, cells are treated with increasing concentrations of palifosfamide lysine in separate plates either as a single-day treatment or three consecutive days of treatment, with fresh drug being added each day. The plates are incubated for 72 h at 37°C with 5% CO2. After 72 h, 250 μg of MTT is added to each well and incubated at 37°C for 6 h. MTT is converted to formazine crystals by mitochondria of viable cells, which are then dissolved in 100 μL of dimethyl sulfoxide. Optical density is measured at 595 nm.
动物实验 Mouse: CB17 female SCID mice are used in the study. Once the tumors reached 50–150 mm3, mice are randomized into control and treatment groups (5-8 mice/group) for each tumor line. Cyclophosphamide is administered at the dose of 150 mg/kg intraperitoneally once a week for 6 weeks. Palifosfamide lysine is administered intravenously at the maximum tolerated dose of 100 mg/kg for three consecutive days as a one-time treatment and serial tumor volumes are determined over the next 6 weeks. Mice are sacrificed at the end of the experiment.
别名 ZIO-201, Isophosphamide mustard, 帕利伐米, Isophosphoramide mustard
分子量 221.02
分子式 C4H11Cl2N2O2P
CAS No. 31645-39-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 42 mg/mL

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TargetMol Library Books参考文献

1. Hingorani P, et al. Preclinical activity of palifosfamide lysine (ZIO-201) in pediatric sarcomas including oxazaphosphorine-resistant osteosarcoma. Cancer Chemother Pharmacol. 2009 Sep;64(4):733-40. 2. Jones B, et al. Anticancer activity of stabilized palifosfamide in vivo: schedule effects, oral bioavailability, and enhanced activity with docetaxel and doxorubicin. Anticancer Drugs. 2012 Feb;23(2):173-84.
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相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 抗癌活性化合物库 酪氨酸激酶分子库 抗癌药物库 药物功能重定位化合物库 已知活性化合物库 经典已知活性库 抗肺癌化合物库 ReFRAME 相关化合物库 表型筛选靶点鉴定库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Palifosfamide 31645-39-3 DNA Damage/DNA Repair Metabolism DNA Alkylator/Crosslinker DNA Alkylation Drug Metabolite ZIO-201 Isophosphamide mustard inhibit ZIO 201 Inhibitor 帕利伐米 Isophosphoramide mustard IPM ZIO201 inhibitor

 

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