1. Cell Cycle/DNA Damage Epigenetics
  2. PARP
  3. AZ9482

AZ9482 是 PARP1/2/6 的三重抑制剂,其对 PARP1/2/6 的IC50 值分别为 1 nM、1 nM 和640 nM。

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AZ9482 Chemical Structure

AZ9482 Chemical Structure

CAS No. : 1825345-33-2

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AZ9482 is a triple PARP1/2/6 inhibitor, with IC50 values of 1 nM, 1 nM and 640 nM for PARP1, PARP2 and PARP6, respectively[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HeLa EC50
< 0.018 μM
Compound: 1; AZ9482
Inhibition of PARP in human HeLa cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis
Inhibition of PARP in human HeLa cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis
[PMID: 26546219]
MCF7 EC50
123 nM
Compound: 1; AZ9482
Inhibition of PARP in multi-drug resistant human MCF7 cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis
Inhibition of PARP in multi-drug resistant human MCF7 cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis
[PMID: 26546219]
MDA-MB-468 EC50
3 nM
Compound: 1; AZ9482
Inhibition of PARP in human MDA-MB-468 cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis
Inhibition of PARP in human MDA-MB-468 cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis
[PMID: 26546219]
OCI-LY19 IC50
0.003 μM
Compound: 1; AZ9482
Cytotoxicity against human OCI-LY19 assessed as growth inhibition after 3 days by Alamar Blue assay
Cytotoxicity against human OCI-LY19 assessed as growth inhibition after 3 days by Alamar Blue assay
[PMID: 26546219]
Sf9 IC50
0.001 μM
Compound: 1; AZ9482
Inhibition of full length human PARP1 expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
Inhibition of full length human PARP1 expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
[PMID: 26546219]
Sf9 IC50
0.001 μM
Compound: 1; AZ9482
Inhibition of human PARP2 (2 to 583 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
Inhibition of human PARP2 (2 to 583 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
[PMID: 26546219]
Sf9 IC50
0.009 μM
Compound: 1; AZ9482
Inhibition of human TNKS1 (1001 to 1327 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
Inhibition of human TNKS1 (1001 to 1327 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
[PMID: 26546219]
Sf9 IC50
0.16 μM
Compound: 1; AZ9482
Inhibition of human TNKS2 (667 to 1166 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
Inhibition of human TNKS2 (667 to 1166 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
[PMID: 26546219]
Sf9 IC50
0.64 μM
Compound: 1; AZ9482
Inhibition of full length human PARP6 expressed in a Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
Inhibition of full length human PARP6 expressed in a Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
[PMID: 26546219]
体外研究
(In Vitro)

AZ9482 exhibits an EC50 of 24 nM in MDA-MB-468 cells[1].
AZ0108 treatment prevents CHK1 MARylation and induces hyperphosphorylation of CHK1, contributing to MPS formation and dysregulation of the cell cycle[1].

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

Cell Viability Assay[1]

Cell Line: MDA-MB-468 cells.
Concentration: 0-10 μM.
Incubation Time: 3 days.
Result: EC50 was 24 nM.
体内研究
(In Vivo)

AZ0108 also displays toxicity in vivo, the molecular basis of which is currently undefined, limiting pharmacological evaluation of AZ0108[1].

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

分子量

450.49

Formula

C26H22N6O2

CAS 号
性状

固体

颜色

White to yellow

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 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 125 mg/mL (277.48 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 2.2198 mL 11.0990 mL 22.1981 mL
5 mM 0.4440 mL 2.2198 mL 4.4396 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。-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: 2.08 mg/mL (4.62 mM); 悬浊液; 超声助溶

    此方案可获得 2.08 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    1 mL 工作液为例,取 100 μL 20.8 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: 2.08 mg/mL (4.62 mM); 悬浊液; 超声助溶

    此方案可获得 2.08 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    1 mL 工作液为例,取 100 μL 20.8 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

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: 98.07%

参考文献

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。-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 2.2198 mL 11.0990 mL 22.1981 mL 55.4951 mL
5 mM 0.4440 mL 2.2198 mL 4.4396 mL 11.0990 mL
10 mM 0.2220 mL 1.1099 mL 2.2198 mL 5.5495 mL
15 mM 0.1480 mL 0.7399 mL 1.4799 mL 3.6997 mL
20 mM 0.1110 mL 0.5550 mL 1.1099 mL 2.7748 mL
25 mM 0.0888 mL 0.4440 mL 0.8879 mL 2.2198 mL
30 mM 0.0740 mL 0.3700 mL 0.7399 mL 1.8498 mL
40 mM 0.0555 mL 0.2775 mL 0.5550 mL 1.3874 mL
50 mM 0.0444 mL 0.2220 mL 0.4440 mL 1.1099 mL
60 mM 0.0370 mL 0.1850 mL 0.3700 mL 0.9249 mL
80 mM 0.0277 mL 0.1387 mL 0.2775 mL 0.6937 mL
100 mM 0.0222 mL 0.1110 mL 0.2220 mL 0.5550 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.

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产品名称:
AZ9482
目录号:
HY-119653
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