AZ9482
目录号 : GC46900
A PARP inhibitor
Cas No.:1825345-33-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
AZ9482 is a poly(ADP-ribose) polymerase (PARP) inhibitor (IC50s = 1, 1, 46, 640, 9, and 160 nM for PARP1, -2, -3, -6, TNKS1/PARP5a, and TNKS2, respectively).1 It induces centrosome declustering (EC50 = <18 nM) and a multipolar spindle phenotype in HeLa cells. AZ9482 inhibits the growth of OCI-LY19 diffuse large B cell lymphoma (DLBCL) cells (GI50 = 3 nM).
1.Johannes, J.W., Almeida, L., Daly, K., et al.Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clusteringBioorg. Med. Chem. Lett.25(24)5743-5747(2015)
| Cas No. | 1825345-33-2 | SDF | |
| Canonical SMILES | O=C1C2=CC=CC=C2C(CC3=CC(C(N4CCN(C5=NC=CC=C5C#N)CC4)=O)=CC=C3)=NN1 | ||
| 分子式 | C26H22N6O2 | 分子量 | 450.5 |
| 溶解度 | DMF: 0.25mg/mL,DMSO: 0.15mg/mL | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2198 mL | 11.0988 mL | 22.1976 mL |
| 5 mM | 0.444 mL | 2.2198 mL | 4.4395 mL |
| 10 mM | 0.222 mL | 1.1099 mL | 2.2198 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Structure-Guided Design and In-Cell Target Profiling of a Cell-Active Target Engagement Probe for PARP Inhibitors
ACS Chem Biol 2020 Feb 21;15(2):325-333.PMID:32017532DOI:PMC7146755
Inhibition of the poly(ADP-ribose) polymerase (PARP) family of enzymes has become an attractive therapeutic strategy in oncology and beyond; however, chemical tools to profile PARP engagement in live cells are lacking. Herein, we report the design and application of PARPYnD, the first photoaffinity probe (AfBP) for PARP enzymes based on triple PARP1/2/6 inhibitor AZ9482, which induces multipolar spindle (MPS) formation in breast cancer cells. PARPYnD is a robust tool for profiling PARP1/2 and is used to profile clinical PARP inhibitor olaparib, identifying several novel off-target proteins. Surprisingly, while PARPYnD can enrich recombinant PARP6 spiked into cellular lysates and inhibits PARP6 in cell-free assays, it does not label PARP6 in intact cells. These data highlight an intriguing biomolecular disparity between recombinant and endogenous PARP6. PARPYnD provides a new approach to expand our knowledge of the targets of this class of compounds and the mechanisms of action of PARP inhibitors in cancer.