PR-104A SN 27858|cas:680199-06-8|西域试剂

PR-104A SN 27858,98.17%

产品编号：Bellancom-14572| CAS NO：680199-06-8| 分子式：C₁₄H₁₉BrN₄O₉S| 分子量：499.29

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-14572	￥4500.00	杭州北京（现货）
Bellancom-14572	￥8000.00	杭州北京（现货）
Bellancom-14572	￥16500.00	杭州北京（现货）
Bellancom-14572	￥25500.00	杭州北京（现货）
Bellancom-14572	￥38000.00	杭州北京（现货）

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PR-104A SN 27858

产品介绍

PR-104A (SN 27858) 是磷酸盐前体 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 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).

体外研究

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.

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

Cell Proliferation Assay

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.

体内研究
(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).

西域 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
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.

体内研究

西域 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
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.

体内研究

西域 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
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.

性状

Solid

溶解性数据

In Vitro:

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

配制储备液

浓度溶剂体积质量	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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 6.25 mg/mL (12.52 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (12.52 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 6.25 mg/mL (12.52 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (12.52 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 6.25 mg/mL (12.52 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (12.52 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。