PR-104A (Synonyms: SN 27858)
目录号: PL04121 纯度: ≥98%
CAS No. :680199-06-8
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中文名称
PR-104A
英文名称
PR-104A
英文别名
2-((2-bromoethyl)-2-{[(2-hydroxyethyl)-amino]-carbonyl}-4,6-dinitroanilino)-ethyl methanesulfonate;PR 104A;SN 27858;2-((2-Bromoethyl)(2-((2-hydroxyethyl)carbamoyl)-4,6-dinitrophenyl)amino)ethyl methanesulfonate;2-((2-bromoethyl)-2-{[(2-hydroxyethyl)amino]carbonyl}-4,6-dinitroanilino)ethyl methanesulfonate;AZICEEZSDKZDHX-UHFFFAOYSA-N
Cas No.
680199-06-8
分子式
C14H19BrN4O9S
分子量
499.29
包装储存
-20°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
产品详情
PR-104A (SN 27858) 是磷酸盐前药 PR-104 的醇代谢物。PR-104A 是一种缺氧选择性的 DNA 交联剂/DNA 损伤剂,也是一种细胞毒素。具有抗肿瘤活性。PR-104A 在缺氧条件下通过 1-电子 NADPH:细胞色素 P450 氧化还原酶代谢。可用于复发/难治性 T 系急性淋巴细胞白血病 (T-ALL) 的研究。
生物活性
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).
性状
Solid
体外研究(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.
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. has not independently confirmed the accuracy of these methods. They are for reference only.
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). has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
参考文献
[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.
溶解度数据
In Vitro: DMSO : 250 mg/mL (500.71 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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