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PR-104A

Cat. No. M3229

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PR-104A Structure
Size Price Availability
5mg USD 220  USD220 Custom Synthesis
10mg USD 300  USD300 Custom Synthesis
50mg USD 780  USD780 Custom Synthesis
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Quality Control & Documentation
Biological Activity

PR-104A is a corresponding alcohol that is systemically converted from PR-104 and a hypoxia-targeted anticancer agent with IC50 of 153 and 60 μM for wild-type CHO AA8 under aerobic and anoxic conditions. PR-104A itself showed modest but significant selectivity for anoxic cells. In a study, the estimated unbound human clearance of PR-104A was 211 L/h/70 kg, with a steady state unbound volume of 105 L/70 kg. The size equivalent unbound PR-104A clearance was 2.5 times faster in dogs, 0.78 times slower in rats and 0.63 times slower in mice, which may reflect reported species differences in PR-104A O-glucuronidation. PR-104A is glucuronidated by UGT2B7 with high specificity and appears to make a major contribution to clearance of PR-104A in humans.

Chemical Information
Molecular Weight 514.33
Formula C15H22BrN4O9S
CAS Number 680199-06-8
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Alessia Stornetta, et al. Drug-DNA adducts as biomarkers for metabolic activation of the nitro-aromatic nitrogen mustard prodrug PR-104A

[2] Stephen M F Jamieson, et al. A novel fluorometric assay for aldo-keto reductase 1C3 predicts metabolic activation of the nitrogen mustard prodrug PR-104A in human leukaemia cells

[3] Christopher P Guise, et al. Diflavin oxidoreductases activate the bioreductive prodrug PR-104A under hypoxia

[4] Yongchuan Gu, et al. Glucuronidation of anticancer prodrug PR-104A: species differences, identification of human UDP-glucuronosyltransferases, and implications for therapy

[5] Yongchuan Gu, et al. Roles of DNA repair and reductase activity in the cytotoxicity of the hypoxia-activated dinitrobenzamide mustard PR-104A

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Keywords: PR-104A supplier, DNA/RNA Synthesis, inhibitors, activators

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