2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. AZD-2461

AZD-2461 是一种有效的 PARP 抑制剂，可抑制 PARP1，PARP2 和 PARP3 的活性，IC50 值分别为 5 nM，2 nM 和 200 nM。

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AZD-2461 Chemical Structure

AZD-2461 Chemical Structure

CAS No. : 1174043-16-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥605
In-stock
5 mg ￥550
In-stock
10 mg ￥800
In-stock
50 mg ￥1500
In-stock
100 mg ￥2495
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

AZD-2461 相关抗体

Top Publications Citing Use of Products

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

AZD-2461 is a potent PARP inhibitor, with IC50s of 5 nM, 2 nM and 200 nM for PARP1, PARP2 and PARP3, respectively.

IC50 & Target[1]

PARP2

2 nM (IC50)

PARP1

5 nM (IC50)

PARP3

200 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HeLa IC50
5 nM
Compound: 96g
Inhibition of human HeLa cell derived PARP preincubated for 10 mins followed by NAD and double stranded DNA-oligos addition and measured after 45 mins by scintillation counting
Inhibition of human HeLa cell derived PARP preincubated for 10 mins followed by NAD and double stranded DNA-oligos addition and measured after 45 mins by scintillation counting
[PMID: 31401008]
MCF-10A IC50
> 50 μM
Compound: Ola
Antiproliferative activity against human MCF-10A cells assessed as cell viability after 72 hrs by MTT assay
Antiproliferative activity against human MCF-10A cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 34455779]
MCF7 IC50
> 50 μM
Compound: Ola
Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 34455779]
MDA-MB-231 IC50
36.92 μM
Compound: Ola
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 34455779]
MDA-MB-468 IC50
35.57 μM
Compound: Ola
Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 34455779]
MEF EC50
14.9 μM
Compound: AZD2461
Cytotoxicity against mouse PARP2 deficient MEF cells expressing PARP1 assessed as reduction in cell viability after 4 to 7 days by cell-titer glo assay
Cytotoxicity against mouse PARP2 deficient MEF cells expressing PARP1 assessed as reduction in cell viability after 4 to 7 days by cell-titer glo assay
[PMID: 29856625]
MEF EC50
22.1 μM
Compound: AZD2461
Cytotoxicity against mouse wild type MEF cells assessed as reduction in cell viability after 4 to 7 days by cell-titer glo assay
Cytotoxicity against mouse wild type MEF cells assessed as reduction in cell viability after 4 to 7 days by cell-titer glo assay
[PMID: 29856625]
MEF EC50
49 μM
Compound: AZD2461
Cytotoxicity against mouse PARP1 deficient MEF cells assessed as reduction in cell viability after 4 to 7 days by cell-titer glo assay
Cytotoxicity against mouse PARP1 deficient MEF cells assessed as reduction in cell viability after 4 to 7 days by cell-titer glo assay
[PMID: 29856625]
体外研究
(In Vitro)

AZD-2461 是一种有效的 PARP 抑制剂，对 PARP1、PARP2 和 PARP3 的 IC50 分别为 5 nM、2 nM 和 200 nM。AZD-2461 (500 nM) 在人 A459 细胞中显示出对 DNA 单链断裂修复的抑制活性。AZD-2461 在 BRCA2 缺陷小鼠乳腺癌细胞系 KB2P3.4中引起耐药性和高 P-gp 表达水平[1]。
AZD-2461 对 BT -20 细胞具有细胞毒性 (5-50 μM)，增加 S 期和 G2 期 BT -20 细胞的比例 (5 -20 μM)，并弱影响 SKBr-3 细胞周期的进程细胞 (5 -20 μM)[2]。

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

AZD-2461 相关抗体:
体内研究
(In Vivo)

AZD-2461 (10 mg/kg，po) 在小鼠结直肠异种移植物中增强替莫唑胺的抗肿瘤活性，并对小鼠骨髓细胞表现出低作用。然而，在大鼠模型中并未观察到 AZD-2461 增加的骨髓耐受性[1]。
AZD-2461 (0.5% v/w HPMC，po) 在短期处理后增加携带 KB1P 肿瘤的小鼠的存活率，长期处理耐受性良好，但不能导致肿瘤根除[3]。

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

395.43

Formula

C22H22FN3O3
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 100 mg/mL (252.89 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5289 mL 12.6445 mL 25.2889 mL
5 mM 0.5058 mL 2.5289 mL 5.0578 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 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: ≥ 2.5 mg/mL (6.32 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (6.32 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 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）。
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

纯度: 99.88%

COA (288 KB) HNMR (278 KB) LCMS (256 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[2]

BT-20 and SKBr-3 human primary breast cancer cell lines are used in the assay. SKBr-3 cells are cultivated in DMEM medium with 10% FCS and BT-20 in RPMI medium under an atmosphere containing 5% CO2. Twenty four hours after plating (at 60-70% confluence), the cells are treated with the PARP-1 inhibitors NU1025, AZD-2461, iniparib, olaparib, and rucaparib at concentrations ranging from 50 to 200 μM, 5 to 50 μM, 5 to 50 μM, 1 to 10 μM, and 0.3 to 10 μM, respectively, for durations indicated in figures 1-7[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Starting from 2 weeks after transplantation into mice, tumor size is monitored at least 3 times a week. All treatments are started when tumors reach a size of approximately 200 mm3. Olaparib (50 mg/kg intraperitoneally) and AZD-2461 (100 mg/kg per os) are given for 28 consecutive days, unless otherwise indicated. If tumors do not shrink below 50% of the initial volume, treatment is continued for another 28 days; otherwise, a new treatment cycle of 28 days is started when the relapsing tumor reaches a size of 100% of the original volume. AZD-2461 is diluted in 0.5% w/v hydroxypropyl methylcellulose in deionized water to a concentration of 10 mg/mL[3].

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

AZD-2461 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5289 mL 12.6445 mL 25.2889 mL 63.2223 mL
5 mM 0.5058 mL 2.5289 mL 5.0578 mL 12.6445 mL
10 mM 0.2529 mL 1.2644 mL 2.5289 mL 6.3222 mL
15 mM 0.1686 mL 0.8430 mL 1.6859 mL 4.2148 mL
20 mM 0.1264 mL 0.6322 mL 1.2644 mL 3.1611 mL
25 mM 0.1012 mL 0.5058 mL 1.0116 mL 2.5289 mL
30 mM 0.0843 mL 0.4215 mL 0.8430 mL 2.1074 mL
40 mM 0.0632 mL 0.3161 mL 0.6322 mL 1.5806 mL
50 mM 0.0506 mL 0.2529 mL 0.5058 mL 1.2644 mL
60 mM 0.0421 mL 0.2107 mL 0.4215 mL 1.0537 mL
80 mM 0.0316 mL 0.1581 mL 0.3161 mL 0.7903 mL
100 mM 0.0253 mL 0.1264 mL 0.2529 mL 0.6322 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:

AZD-24611174043-16-3AZD2461AZD 2461PARPpoly ADP ribose polymeraseInhibitorinhibitorinhibit

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