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Related CAS#:
31645-39-3 1070409-31-2

31645-39-3

31645-39-3 structure
31645-39-3 structure
Name Palifosfamide
Synonyms Phosphorodiamidic acid, N,N'-bis(2-chloroethyl)-
Isophosphamide mustard
Ipam
Ifosforamide mustard
N,N'-Bis(2-chloroethyl)phosphorodiamidic acid
ifosfamide mustard
isophosphoramide mustard
isophosphoramide
isophpsphoramide mustard
Palifosfamide
Description Palifosfamide is a novel DNA alkylator and the active metabolite of ifosfamide, with antitumor activity.
Related Catalog
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].
Cell Assay 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 Admin 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.

[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.
Density 1.4±0.1 g/cm3
Boiling Point 341.5±52.0 °C at 760 mmHg
Melting Point 106-107ºC
Molecular Formula C4H11Cl2N2O2P
Molecular Weight 221.022
Flash Point 160.4±30.7 °C
Exact Mass 219.993515
PSA 71.17000
LogP -1.05
Appearance white solid
Vapour Pressure 0.0±1.6 mmHg at 25°C
Index of Refraction 1.498
Storage condition -20℃

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title: CAS No. 31645-39-3 | Chemsrc address: https://www.chemsrc.com/en/baike/918884.html

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