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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
CAS NO:2337386-47-5
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
CAY10749 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively . CAY10749 是一种针对多种肿瘤疾病的高效抗癌化合物。
Cas No.2337386-47-5
Canonical SMILESO=C1C2=CC=CC=C2C(CC3=CC(C(N4CC5=NC(C6=CN=C(N)C=C6C(F)(F)F)=NC(N7CCOCC7)=C5CC4)=O)=C(F)C=C3)=NN1
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
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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)