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
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
More Info
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.
Biological target:
LSZ-102 is a potent, orally bioavailable selective estrogen receptor degrader with an IC50 of 0.2 nM.
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
100.0 |
212.56 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
470.46
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
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
