帕利伐米 T4350

Product Introduction
Bioactivity


英文名: Palifosfamide

描述: 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。

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.

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.

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

溶解度: DMSO : < 1mg/ml (insoluble）


关键字: inhibit | ZIO 201 | DNA Alkylator/Crosslinker | Inhibitor | Drug Metabolite | IPM | Palifosfamide | ZIO201

相关产品: Altretamine | Lomustine | RITA | Thio-TEPA | Miriplatin | Chlorambucil | Oxaliplatin | Treosulfan | Cisplatin | PK11000

相关库: Anti-Aging Compound Library | Drug Repurposing Compound Library | ReFRAME Related Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Anti-Lung Cancer Compound Library | Human Metabolite Library | Anti-Cancer Clinical Compound Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound Library

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