Chemical Structure : PR-104
CAS No.:
851627-62-8
PR-104
(PR104)
Catalog No.: PC-23371Not For Human Use, Lab Use Only.
PR-104 is a hypoxia-activated DNA cross-linking agent and phosphate ester of the nitrogen mustard prodrug PR-104A, shows selective DNA cross-linking selective cytotoxicity under hypoxia in cancer cells.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
PR-104 is a hypoxia-activated DNA cross-linking agent and phosphate ester of the nitrogen mustard prodrug PR-104A, shows selective DNA cross-linking selective cytotoxicity under hypoxia in cancer cells.
The cytotoxicity of PR-104A was increased 10- to 100-fold by hypoxia in vitro.
PR-104 is reduced to activated DNA cross-linking metabolites (hydroxylamine PR-104H and amine PR-104M) under hypoxia by one-electron reductases and independently of hypoxia by the 2-electron reductase aldo-keto reductase 1C3 (AKR1C3).
Overexpression of AKR1C3 in a resistant BCP-ALL xenograft resulted in dramatic sensitization to PR-104 in vivo.
PR-104 showed significantly greater efficacy against T-lineage ALL (T-ALL) than B-cell-precursor ALL (BCP-ALL) xenografts.
Physicochemical Properties
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M.Wt
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579.27
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Formula
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C14H20BrN4O12PS
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-((2-bromoethyl)(2,4-dinitro-6-((2-(phosphonooxy)ethyl)carbamoyl)phenyl)amino)ethyl methanesulfonate
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References
1. Moradi Manesh D, et al. Blood. 2015 Sep 3;126(10):1193-202.
2. McKeage MJ, et al. BMC Cancer. 2012 Oct 25;12:496.
3. Adam V Patterson, et al. Clin Cancer Res. 2007 Jul 1;13(13):3922-32.
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