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CAY10749
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAY10749图片
规格:98%
分子量:660.6
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
A dual inhibitor of PARP and PI3K
货号:ajcx22024
CAS:2337386-47-5
分子式:C33H28F4N8O3
分子量:660.6
溶解度:DMF: 11mg/mL,DMF:PBS (pH 7.2) (1:2): 0.3mg/mL,DMSO: 10mg/mL
纯度:98%
存储:Store at -20°C
库存:现货

Background:

CAY10749 is a dual inhibitor of poly(ADP-ribose) polymerase (PARP) and PI3K (IC50s = 6.03, 3.63, 5.62, and 7.41 nM for PARP1, PARP2, PI3Kα, and PI3Kδ, respectively).1It is selective for these enzymes over PI3Kβ and PI3Kγ (IC50s = 288.4 and 831.76 nM, respectively), as well as a panel of 374 additional kinases at 1 µM. CAY10749 (1 µM) induces dsDNA break formation in a neutral comet assay and apoptosis in MDA-MB-468 breast cancer cells. It inhibits proliferation of eight cancer cell lines, including pancreatic, ovarian, lymphoma, leukemia, and lung cancer cells, with IC50values ranging from 398.11 to 2,818.38 nM. CAY10749 (50 mg/kg twice per day) reduces tumor growth by 73.4% in an MDA-MB-468 mouse xenograft model.


1.Wang, J., Li, H., He, G., et al.Discovery of novel dual poly(ADP-ribose)polymerase (PARP) and phosphoinositide 3-kinase (PI3K) inhibitors as a promising strategy for cancer therapyJ. Med. Chem.63(1)122-139(2019)