PR-104A (Synonyms: SN 27858) |
| カタログ番号GC62490 |
PR-104A (SN 27858) は、リン酸プロドラッグ PR-104 のアルコール代謝物です。 PR-104A は、低酸素選択的 DNA 架橋剤/DNA 損傷剤および細胞毒素です。抗腫瘍活性。 PR-104A は、低酸素下で 1 電子 NADPH:チトクローム P450 オキシドレダクターゼによって代謝されます。 PR-104A は、再発・難治性の T 系統急性リンパ性白血病 (T-ALL) の研究に使用できます。
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Cas No.: 680199-06-8
Sample solution is provided at 25 µL, 10mM.
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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].
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 "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].
[1]. Adam V Patterson, et al. Mechanism of action and preclinical antitumor activity of the novel hypoxia-activated DNA cross-linking agent PR-104. Clin Cancer Res. 2007 Jul 1;13(13):3922-32.
[2]. Donya Moradi Manesh, et al. AKR1C3 is a biomarker of sensitivity to PR-104 in preclinical models of T-cell acute lymphoblastic leukemia. Blood. 2015 Sep 3;126(10):1193-202.
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