ZB716, formerly known as fulvestrant-3-boronic acid, is a synthetic, steroidal, orally bioavailableantiestrogen which is under development for the treatment of estrogen receptor (ER)-positive metastatic breast cancer. The drug is a silent antagonist of the ERα (IC50 = 4.1 nM) as well as a selective estrogen receptor degrader (SERD). It is an analogue of fulvestrant in which the C3 hydroxyl group has been replaced with a boronic acidmoiety. In accordance, the two drugs have similar pharmacodynamic properties. However, whereas fulvestrant is not orally bioavailable and must be administered via intramuscular injection, ZB716 is less susceptible to first-pass metabolism, and in relation to this, is orally bioavailable. References: Guo S, Zhang C, Bratton M, Mottamal M, Liu J, Ma P, Zheng S, Zhong Q, Yang L, Wiese TE, Wu Y, Ellis MJ, Matossian M, Burow ME, Miele L, Houtman R, Wang G. ZB716, a steroidal selective estrogen receptor degrader (SERD), is orally efficacious in blocking tumor growth in mouse xenograft models. Oncotarget. 2018 Jan 8;9(6):6924-6937. doi: 10.18632/oncotarget.24023. eCollection 2018 Jan 23. PubMed PMID: 29467940; PubMed Central PMCID: PMC5805526.

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CAS：1853279-29-4