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

PR-104A (SN 27858) is the alcohol metabolite of phosphate proagent 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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 494 In-stock
Solution
10 mM * 1 mL in DMSO USD 494 In-stock
Solid
5 mg USD 450 In-stock
10 mg USD 800 In-stock
25 mg USD 1650 In-stock
50 mg USD 2550 In-stock
100 mg USD 3800 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PR-104A (SN 27858) is the alcohol metabolite of phosphate proagent 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].

MedChemExpress (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].

MedChemExpress (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.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

BrCCN(CCOS(=O)(C)=O)C1=C(C(NCCO)=O)C=C([N+]([O-])=O)C=C1[N+]([O-])=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (500.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
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Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.17%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0028 mL 10.0142 mL 20.0284 mL 50.0711 mL
5 mM 0.4006 mL 2.0028 mL 4.0057 mL 10.0142 mL
10 mM 0.2003 mL 1.0014 mL 2.0028 mL 5.0071 mL
15 mM 0.1335 mL 0.6676 mL 1.3352 mL 3.3381 mL
20 mM 0.1001 mL 0.5007 mL 1.0014 mL 2.5036 mL
25 mM 0.0801 mL 0.4006 mL 0.8011 mL 2.0028 mL
30 mM 0.0668 mL 0.3338 mL 0.6676 mL 1.6690 mL
40 mM 0.0501 mL 0.2504 mL 0.5007 mL 1.2518 mL
50 mM 0.0401 mL 0.2003 mL 0.4006 mL 1.0014 mL
60 mM 0.0334 mL 0.1669 mL 0.3338 mL 0.8345 mL
80 mM 0.0250 mL 0.1252 mL 0.2504 mL 0.6259 mL
100 mM 0.0200 mL 0.1001 mL 0.2003 mL 0.5007 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PR-104A
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