LSZ102
LSZ102 is a potent ERα antagonist and degrader. LSZ102 showed ERα degradation IC50 = 0.2 nM. LSZ102 demonstrated IC50 for MCF-7 cells = 1.7 nM. Upon administration of LSZ102, this agent binds to the ER and induces the degradation of the receptor. This prevents ER activation and ER-mediated signaling, and inhibits the growth and survival of ER-expressing cancer cells.
For research use only. We do not sell to patients.
Chemical Information
| Name | LSZ102 |
|---|---|
| Iupac Chemical Name | (E) -3- (4-((2-(2- (1,1-Difluoroethyl)-4-fluorophenyl)-6-hydroxybenzo[b]thiophen-3-yl)oxy)phenyl)acrylic Acid |
| Synonyms | LSZ102; LSZ-102; LSZ 102; SERD LSZ102; SERD LSZ-102; SERD LSZ 102; |
| Molecular Formula | C25H17F3O4S |
| Molecular Weight | 470.4622 |
| Smile | O=C(O)/C=C/C1=CC=C(OC2=C(C3=CC=C(F)C=C3C(F)(F)C)SC4=CC(O)=CC=C42)C=C1 |
| InChiKey | SJXNPGGVGZXKKI-NYYWCZLTSA-N |
| InChi | InChI=1S/C25H17F3O4S/c1-25(27,28)20-12-15(26)5-9-18(20)24-23(19-10-6-16(29)13-21(19)33-24)32-17-7-2-14(3-8-17)4-11-22(30)31/h2-13,29H,1H3,(H,30,31)/b11-4+ |
| CAS Number | 2135600-76-7 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer
George S. Tria, Tinya Abrams, Jason Baird, Heather E. Burks, Brant Firestone, L. Alex Gaither, Lawrence G. Hamann, Guo He, Christina A. Kirby, Sunkyu Kim, Franco Lombardo, Kaitlin J. Macchi, Donald P. McDonnell, Yuji Mishina, John D. Norris, Jill Nunez, Clayton Springer, Yingchuan Sun, Noel M. Thomsen, Chunrong Wang, Jianling Wang, Bing Yu, Choi-Lai Tiong-Yip and Stefan Peukert
Publication Date (Web): March 22, 2018 (Article)
DOI: 10.1021/acs.jmedchem.7b01682
Chemical Structure
