1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
  2. DNA Alkylator/Crosslinker
    Drug Metabolite
  3. PR-104A

PR-104A (Synonyms: SN 27858)

Cat. No.: HY-14572
Handling Instructions

PR-104A (SN 27858) is the alcohol metabolite of phosphate prodrug PR-104. PR-104A is a hypoxia-selective DNA cross-linking agent/DNA-damaging agent and cytotoxin. Antitumor Activity. PR-104A is metabolized under hypoxia by the 1-electron NADPH:cytochrome P450 oxidoreductase. PR-104A can be used for the research of relapsed/refractory T-lineage acute lymphoblastic leukemia (T-ALL).

For research use only. We do not sell to patients.

PR-104A Chemical Structure

PR-104A Chemical Structure

CAS No. : 680199-06-8

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 494 In-stock
Estimated Time of Arrival: December 31
Oil + Solvent
10 mM * 1 mL
ready for reconstitution
USD 494 In-stock
Estimated Time of Arrival: December 31
Oil
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 800 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2550 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3800 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

PR-104A (SN 27858) is the alcohol metabolite of phosphate prodrug PR-104. PR-104A is a hypoxia-selective DNA cross-linking agent/DNA-damaging agent and cytotoxin. Antitumor Activity[1]. PR-104A is metabolized under hypoxia by the 1-electron NADPH:cytochrome P450 oxidoreductase. PR-104A can be used for the research of relapsed/refractory T-lineage acute lymphoblastic leukemia (T-ALL)[2].

In Vitro

PR-104A (1-100 uM) shows antiproliferative potency in a panel of 10 human carcinoma cell lines following 4 hours exposures under aerobic and hypoxic conditions with the lowest IC50 (0.51 μM) in H460 non–small cell lung cancer cells and highest (7.3 μM) in PC3 prostate cells[1].
The phosphate ester PR-104 is rapidly converted in vivo to the alcohol PR-104A, a nitrogen mustard prodrug that is metabolised to hydroxylamine (PR-104H) and amine (PR-104M) DNA crosslinking agents by one-electron reductases in hypoxic cells and by aldo-keto reductase 1C3 independently of oxygen[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: HT29 , HCT116, C33A SiHa A549, H460, H1299 ,PC3,SKOV3, A375 cells
Concentration: 0, 1, 10, 100 uM
Incubation Time: 4 hours under aerobic or hypoxic conditions
Result: The lowest IC50 (0.51 μM) in H460 non-small cell lung cancer cells and highest (7.3 μM) in PC3 prostate cells.
In Vivo

The phosphate ester “pre-prodrug” PR-104 is well tolerated in mice and converted rapidly to the corresponding prodrug PR-104A. H460 xenografts shows significant sensitivity to PR-104 (total dose 3.2 mmol/kg)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Specific pathogen-free homozygous nude (CD1-Foxn1nu) mice with H460 xenografts[1]
Dosage: Daily (0.23 mmol/kg/dose; qd ×14) or weekly (1.07 mmol/kg/dose; qw ×3)
Administration: I.p.
Result: The single-agent activity against H460 tumors refractory to docetaxel, cisplatin, gemcitabine, and cyclophosphamide was particularly striking.
Compared a daily (qd ×14) versus weekly (qw ×3) schedule against the chemoresistant H460 xenograft model using the same total dose (3.2 mmol/kg) over 14 days, which was well tolerated using both schedules.
Molecular Weight

499.29

Formula

C₁₄H₁₉BrN₄O₉S

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (500.71 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0028 mL 10.0142 mL 20.0284 mL
5 mM 0.4006 mL 2.0028 mL 4.0057 mL
10 mM 0.2003 mL 1.0014 mL 2.0028 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 6.25 mg/mL (12.52 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 6.25 mg/mL (12.52 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 6.25 mg/mL (12.52 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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PR-104A
Cat. No.:
HY-14572
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