Palifosfamide (Synonyms: Isophosphoramide Mustard, NSC 297900) |
| カタログ番号GC14762 |
イホスファミドの活性代謝物質
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 31645-39-3
Sample solution is provided at 25 µL, 10mM.
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Palifosfamide is the active moiety of ifosfamide (IFA) [1].
IFA is alkylating agents which are active against a variety of pediatric sarcomas such as rhabdomyosarcoma (RMS), Ewing's sarcoma (ES), osteosarcoma (OS) and other undifferentiated soft tissue sarcomas [1].
In human OS cell lines SaOS-2, OS229 and OS230, Palifosfamide lysine has broad activity with IC50 ranging from 2.25 to 6.75 μM. While OS222 had the IC50 of 31.5 μM [1].
In CB17 female SCID mice, palifosfamide lysine (100 mg/kg) administered intravenously for three consecutive days, the mean weight loss was less than 15% and complete recovery to baseline within 4 weeks of treatment. While, doses higher than 100 mg/kg for three consecutive days lead to either greater than 20% loss of body weight or death. In NCr-nu/nu mice bearing established orthotopic mammary MX-1 tumor xenografts, palifosfamide suppressed MX-1 tumor growth by greater than 80% with 17% complete antitumor responses [2].
References:
[1]. Hingorani P, Zhang W, Piperdi S, et al. Preclinical activity of palifosfamide lysine (ZIO-201) in pediatric sarcomas including oxazaphosphorine-resistant osteosarcoma. Cancer Chemother Pharmacol, 2009, 64(4): 733-740.
[2]. Jones B, Komarnitsky P, Miller GT, et al. Anticancer activity of stabilized palifosfamide in vivo: schedule effects, oral bioavailability, and enhanced activity with docetaxel and doxorubicin. Anticancer Drugs, 2012, 23(2): 173-184.
Cell experiment: | 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]. |
Animal experiment: | 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]. |
References: [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. | |
| Cas No. | 31645-39-3 | SDF | |
| 同義語 | Isophosphoramide Mustard, NSC 297900 | ||
| Chemical Name | bis(2-chloroethylamino)phosphinic acid | ||
| Canonical SMILES | C(CCl)NP(=O)(NCCCl)O | ||
| Formula | C4H11Cl2N2O2P | M.Wt | 221.02 |
| 溶解度 | ≥ 22.1 mg/mL in DMSO, ≥ 19.4 mg/mL in Water with ultrasonic and warming | Storage | Store at -20°C, protect from light, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 | 9.049 mL |
| 10 mM | 0.4524 mL | 2.2622 mL | 4.5245 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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