1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
  2. DNA Alkylator/Crosslinker
    Drug Metabolite
  3. Palifosfamide

Palifosfamide (Synonyms: Isophosphoramide mustard; IPM; ZIO-201)

Cat. No.: HY-14798
Handling Instructions

Palifosfamide is a novel DNA alkylator and the active metabolite of ifosfamide, with antitumor activity.

For research use only. We do not sell to patients.

Palifosfamide Chemical Structure

Palifosfamide Chemical Structure

CAS No. : 31645-39-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 330 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 432 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1164 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Palifosfamide is a novel DNA alkylator and the active metabolite of ifosfamide, with antitumor activity.

In Vitro

Palifosfamide 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 ro 6.75 μM for most cell lines except OS222 (IC50=31.5 μM)[1].

In Vivo

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[1]. 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[2].

Clinical Trial
Molecular Weight

221.02

Formula

C₄H₁₁Cl₂N₂O₂P

CAS No.

31645-39-3

SMILES

O=P(NCCCl)(NCCCl)O

Shipping

Room temperature in continental US; may vary elsewhere

Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 42 mg/mL (190.03 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.5245 mL 22.6224 mL 45.2448 mL
5 mM 0.9049 mL 4.5245 mL 9.0490 mL
10 mM 0.4524 mL 2.2622 mL 4.5245 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice: 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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Palifosfamide
Cat. No.:
HY-14798
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