1. Cell Cycle/DNA Damage
  2. DNA Alkylator/Crosslinker
  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

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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].

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.
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

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

PR-104ASN 27858SN27858SN-27858DNA Alkylator/CrosslinkeralcoholmetabolitehypoxiaDNAcross-linkingdamagingcytotoxinNADPHcytochromeP450oxidoreductaserelapsedrefractoryT-lineageacutelymphoblasticleukemiaT-ALLInhibitorinhibitorinhibit

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