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Palifosfamide

SKU: orb1302928

Description

Palifosfamide lysine (ZIO-201) is a stabilized derivative of isophosphoramide mustard with broad-spectrum in vitro activity against sarcoma cell lines, typically exhibiting IC50 values in the low micromolar range. It has been investigated in preclinical sarcoma models and has progressed to clinical trials for soft tissue sarcoma, demonstrating its relevance for oncology research.
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Research Area

Metabolism Research, Molecular Biology

Images & Validation

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Palifosfamide

Key Properties

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CAS Number31645-39-3
MW221.02
Purity99.72% (May vary between batches)
FormulaC4H11Cl2N2O2P
SMILESP(NCCCl)(NCCCl)(=O)O
TargetDNA Alkylation,DNA Alkylator/Crosslinker,Drug Metabolite
SolubilityDMSO:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

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Target IC50
OS222:31.5 μM
In Vitro
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.
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Cell Research
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.
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Animal Research
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.
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Storage & Handling

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StoragePure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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ZIO 201, ZIO201, ZIO-201, Inhibitor, IPM, Isophosphamide mustard, Isophosphoramide mustard, inhibit, Palifosfamide, Crosslinker, DNAAlkylator, DNAAlkylation, DNA Alkylation, DNA Alkylator, DNA alkylator, DNA Alkylator/Crosslinker, DrugMetabolite, Drug Metabolite

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    Palifosfamide [orb1223154]

    >98% (HPLC)

    31645-39-3

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    C4H11Cl2N2O2P

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Compound Identifiers

PubChem CID
100427 ↗

Key Properties

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No computed properties available.

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Palifosfamide (orb1302928)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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1 mg
$ 110.00
2 mg
$ 140.00
5 mg
$ 220.00
10 mg
$ 330.00
25 mg
$ 500.00
50 mg
$ 640.00
100 mg
$ 910.00
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