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

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。

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PR-104A Chemical Structure

PR-104A Chemical Structure

CAS No. : 680199-06-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3080
In-stock
5 mg ￥2800
In-stock
10 mg ￥4500
In-stock
25 mg 现货 询价
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100 mg   询价  

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Customer Review

PR-104A 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[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].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
DU-145 IC50
210 μM
Compound: 16; PR104A
Cytotoxicity against human DU145 cells assessed as reduction in cell viability incubated for 2 hrs under normoxic condition followed by washed with fresh media incubated for 3 days by alamar blue assay
Cytotoxicity against human DU145 cells assessed as reduction in cell viability incubated for 2 hrs under normoxic condition followed by washed with fresh media incubated for 3 days by alamar blue assay
[PMID: 33220402]
DU-145 IC50
78 μM
Compound: 16; PR104A
Cytotoxicity against human DU145 cells assessed as reduction in cell viability incubated for 2 hrs under hypoxic condition followed washed with fresh media incubated for 3 days by alamar blue assay
Cytotoxicity against human DU145 cells assessed as reduction in cell viability incubated for 2 hrs under hypoxic condition followed washed with fresh media incubated for 3 days by alamar blue assay
[PMID: 33220402]
PC-3 IC50
320 μM
Compound: 16; PR104A
Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 2 hrs under normoxic condition followed by washed with fresh media incubated for 3 days by alamar blue assay
Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 2 hrs under normoxic condition followed by washed with fresh media incubated for 3 days by alamar blue assay
[PMID: 33220402]
PC-3 IC50
48 μM
Compound: 16; PR104A
Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 2 hrs under hypoxic condition followed by washed with fresh media incubated for 3 days by alamar blue assay
Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 2 hrs under hypoxic condition followed by washed with fresh media incubated for 3 days by alamar blue assay
[PMID: 33220402]
PC-3 IC50
7.3 μM
Compound: 16; PR104A
Cytotoxicity against human PC-3 cells assessed as reduction in cell viability preincubated for 4 hrs in hypoxia and further incubated for 5 days in fresh medium by SRB assay
Cytotoxicity against human PC-3 cells assessed as reduction in cell viability preincubated for 4 hrs in hypoxia and further incubated for 5 days in fresh medium by SRB assay
[PMID: 33220402]
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[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].

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

PR-104A 相关抗体:

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.
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)[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.
分子量

499.29

Formula

C14H19BrN4O9S
CAS 号
性状

固体

颜色

Light yellow to green yellow

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)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (200.28 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

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

  • 方案 一

    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); 澄清溶液

    此方案可获得 ≥ 6.25 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    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); 澄清溶液

    此方案可获得 ≥ 6.25 mg/mL（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。

    2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。

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

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献

PR-104A 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 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
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.

Keywords:

PR-104A680199-06-8SN 27858SN27858SN-27858DNA Alkylator/CrosslinkerDrug MetabolitealcoholmetabolitehypoxiaDNAcross-linkingdamagingcytotoxinNADPHcytochromeP450oxidoreductaserelapsedrefractoryT-lineageacutelymphoblasticleukemiaT-ALLInhibitorinhibitorinhibit

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