WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206950
CAS#: 2135600-76-7
Description: 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.
MedKoo Cat#: 206950
Name: LSZ102
CAS#: 2135600-76-7
Chemical Formula: C25H17F3O4S
Exact Mass: 470.08
Molecular Weight: 470.4622
Elemental Analysis: C, 63.83; H, 3.64; F, 12.11; O, 13.60; S, 6.81
Synonym: LSZ102; LSZ-102; LSZ 102; SERD LSZ102; SERD LSZ-102; SERD LSZ 102;
IUPAC/Chemical Name: (E) -3- (4-((2-(2- (1,1-Difluoroethyl)-4-fluorophenyl)-6-hydroxybenzo[b]thiophen-3-yl)oxy)phenyl)acrylic Acid
InChi Key: SJXNPGGVGZXKKI-NYYWCZLTSA-N
InChi Code: 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+
SMILES Code: 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
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
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.
Storage Condition: 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
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
| Biological target: | LSZ-102 is a potent, orally bioavailable selective estrogen receptor degrader with an IC50 of 0.2 nM. |
| In vitro activity: | TBD |
| In vivo activity: | TBD |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 100.0 | 212.56 |
The following data is based on the product molecular weight 470.4622 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | TBD |
| In vitro protocol: | TBD |
| In vivo protocol: | TBD |
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
LSZ102 is currently being evaluated in advanced or metastatic ERα+ breast cancer in a Phase I/Ib trial. Preliminary results from this study indicate that oral single-agent LSZ102 appears well-tolerated, with a manageable safety profile.
