COA of Formula: C7H13BrO2. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 2-(2-Bromoethoxy)tetrahydro-2H-pyran, is researched, Molecular C7H13BrO2, CAS is 17739-45-6, about Discovery of Pamiparib (BGB-290), a Potent and Selective Poly (ADP-ribose) Polymerase (PARP) Inhibitor in Clinical Development. Author is Wang, Hexiang; Ren, Bo; Liu, Ye; Jiang, Beibei; Guo, Yin; Wei, Min; Luo, Lusong; Kuang, Xianzhao; Qiu, Ming; Lv, Lei; Xu, Hong; Qi, Ruipeng; Yan, Huibin; Xu, Dexu; Wang, Zhiwei; Huo, Chang-Xin; Zhu, Yutong; Zhao, Yuan; Wu, Yiyuan; Qin, Zhen; Su, Dan; Tang, Tristin; Wang, Fan; Sun, Xuebing; Feng, Yingcai; Peng, Hao; Wang, Xing; Gao, Yajuan; Liu, Yong; Gong, Wenfeng; Yu, Fenglong; Liu, Xuesong; Wang, Lai; Zhou, Changyou.
Poly (ADP-ribose) polymerase (PARP) plays a significant role in DNA repair responses; therefore, this enzyme is targeted by PARP inhibitors in cancer therapy. Here we have developed a number of fused tetra- or pentacyclic dihydrodiazepinoindolone derivatives with excellent PARP enzymic and cellular PARylation inhibition activities. These efforts led to the identification of pamiparib (BGB-290, 139), which displays excellent PARP-1 and PARP-2 inhibition with IC50 of 1.3 and 0.9 nM, resp. In a cellular PARylation assay, this compound inhibits PARP activity with IC50 = 0.2 nM. Cocrystal of pamiparib shows similar binding sites with PARP with other PARP inhibitors, but pamiparib is not a P-gp substrate and shows excellent drug metabolism and pharmacokinetics (DMPK) properties with significant brain penetration (17-19%, mice). The compound is currently being investigated in phase III clin. trials as a maintenance therapy in platinum-sensitive ovarian cancer and gastric cancer.
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Reference:
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