公告提醒：爱必信所有产品和服务仅用于科学研究，不用于临床应用及其他用途提供产品和服务（也不为任何个人提供产品和服务）!
YZ剂描述： 产品名称：Veliparib (ABT-888) 产品别名：2-[(2R)-2-甲基-2-烷基]-1H-苯并咪唑-7-甲酰胺 英文别名：ABT-888;ABT 888;ABT888;NSC 737664 靶点：PARP2 ,PARP1 CAS：912444-00-9 纯度：98% min 外观：见爱必信官网 保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months. 描述： Veliparib (ABT-888)是一种有效的PARP1和PARP2YZ剂，无细胞试验中Ki分别为5.2 nM和2.9 nM，对SIRT2没有活性。 溶解性：DMSO Solubility: 17 mg/mL (69.58 mM) 体外研究： ABT-888 is inactive to SIRT2 (>5 μM). ABT-888 inhibits the PARP activity with EC50 of 2 nM in C41 cells. ABT-888 could decrease the PAR levels in both irradiated and nonirradiated H460 cells. ABT-888 also reduces clonogenic survival and inhibits DNA repair by PARP-1 inhibition in H460 cells. ABT-888 increases apoptosis and autophagy in H460 cells when combination with radiation. ABT-888 also inhibits PARP activity in H1299, DU145 and 22RV1 cells and the inhibition is independent of p53 function. ABT-888 (10 μM) suppresses the surviving fraction (SF) by 43% in the clonogenic H1299 cells. ABT-888 shows effective radiosensitivity in oxic H1299 cells. Furthermore, ABT-888 could attenuate the SF of hypoxic-irradiated cells including H1299, DU145 and 22RV1. 体内研究：The oral bioavailability of ABT-888 is 56%-92% in mice, Sprague-Dawley rats, beagle dogs, and cynomolgus monkeys after oral administration. ABT-888 (25 mg/kg i.p.) could improve tumor growth delay in a NCI-H460 xenograft model with well tolerated. Combination with radiation, ABT-888 decreases the tumor vessel formation. ABT-888 reduces intratumor PAR levels by more than 95% at a dose of 3 and 12.5 mg/kg in A375 and Colo829 xenograft models and the suppression could be maintained over time. 产品信息订购：
产品更多信息请进入爱必信网站咨询 |
