ZB716

• CAT Number: I038665
• CAS Number: 1853279-29-4
• Molecular Formula: C32H48BF5O4S
• Molecular Weight: 634.59
• Purity: ≥95%
• IUPAC Name: [(7R,8R,9S,13S,14S,17S)-17-hydroxy-13-methyl-7-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl]-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-3-yl]boronic acid
• InChI: InChI=1S/C32H48BF5O4S/c1-30-17-15-26-25-12-11-24(33(40)41)21-23(25)20-22(29(26)27(30)13-14-28(30)39)10-7-5-3-2-4-6-8-18-43(42)19-9-16-31(34,35)32(36,37)38/h11-12,21-22,26-29,39-41H,2-10,13-20H2,1H3/t22-,26-,27+,28+,29-,30+,43?/m1/s1
• SMILES: B(C1=CC2=C(C=C1)[C@H]3CC[C@]4([C@H]([C@@H]3[C@@H](C2)CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F)CC[C@@H]4O)C)(O)O

ZB716 is a steroidal, orally bioavailable SERD (selective estrogen receptor downregulator) that binds to ER with high affinity and exerts its antiestrogenic effect on ER-expressing breast cancer cells. In both tamoxifen-naive and tamoxifen-resistant breast cancer cells, ZB716 potently inhibits cell proliferation and effectively degrades the hormone receptor in a dose-dependent manner. ZB716 is shown to have far superior oral bioavailability in mice when compared to fulvestrant.
* Sold in collaboration with Zenopharm, LLC
KEYWORDS: ZB716 | supplier | SERD | ZB-716 | CAS [1853279-29-4] | Estrogen | Estrogen (ER) | Downregulator | selective estrogen receptor downregulator | nuclear | steroidal | breast cancer | cell proliferation

Reference

J Liu et al. Fulvestrant-3 Boronic Acid (ZB716): An Orally Bioavailable Selective Estrogen Receptor Downregulator (SERD). J Med Chem. 2016 Sep 8;59(17):8134-40.

J Liu et al. Fulvestrant-3-Boronic Acid (ZB716) Demonstrates Oral Bioavailability and Favorable Pharmacokinetic Profile in Preclinical ADME Studies. Pharmaceuticals (Basel). 2021 Jul 26;14(8):719.