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ZB716
- Borestrant
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C32H48BF5O4S
- MW: 634.59
Description
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
More Information
| Parent CAS No. | 1853279-29-4 |
|---|---|
| Chemical Name | (7R,8R,9S,13S,14S,17S)-17-hydroxy-13-methyl-7-(9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-3-ylboronic acid |
| extra_info | * Sold in collaboration with Zenopharm, LLC |
| SMILES | C1C=C2[C@@]3([H])CC[C@]4(C)[C@@H](O)CC[C@@]4([H])[C@]3([H])[C@H](CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F)CC2=CC=1B(O)O |&1:3,7,9,13,15,17,r| |
| MFCD | N.A. |
| 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 |
| InChiKey | FIAYIYKWRBIBQG-GDWZZRAASA-N |
| CID | 126480615 |
| Short Description | SERD |
References
- 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.
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