Free shipping on all orders over $ 500

PR-104A

Cat. No. M3229

All AbMole products are for research use only, cannot be used for human consumption.

PR-104A Structure
Size Price Availability
5mg USD 220  USD220 Custom Synthesis
10mg USD 300  USD300 Custom Synthesis
50mg USD 780  USD780 Custom Synthesis
Free Delivery on orders over USD 500 Bulk Inquiry?

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

Related DNA/RNA Synthesis Products
GSK4418959

GSK4418959 (IDE275) is a non-covalent, reversible, selective and orally active WRN helicase inhibitor. GSK4418959 inhibits ATPase and DNA unwinding functions in an ATP-competitive manner.

Dencatistat

Dencatistat (P115) is an inhibitor of Cytidine Triphosphate Synthase 1 (CTPS1) with an IC50 value of ≤ 0.1 μM.

Antipain dihydrochloride

Antipain dihydrochloride is a protease inhibitor. Antipain dihydrochloride inhibits N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation and increases chromosomal aberrations. Antipain dihydrochloride also restricts uterine DNA synthesis and function in mice.

Tetrahydrouridine

Tetrahydrouridine (THU) is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine.

Crisnatol

Crisnatol (BWA770U) is a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol shows in vitro cytotoxicity against human breast cancer cells. Crisnatol (BWA770U) is also an orally active and anticancer agent.

  Catalog
Abmole Inhibitor Catalog




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

All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.



Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.