Specification
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.
Synonyms
LSZ102; LSZ-102; LSZ 102; SERD LSZ102; SERD LSZ-102; SERD LSZ 102
IUPAC Name
(E) -3- (4-((2-(2- (1,1-Difluoroethyl)-4-fluorophenyl)-6-hydroxybenzo[b]thiophen-3-yl)oxy)phenyl)acrylic Acid
Canonical SMILES
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
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+
InChI Key
SJXNPGGVGZXKKI-NYYWCZLTSA-N
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Storage
Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Drug Formulation
This drug may be formulated in DMSO
Elemental Analysis
C, 63.83; H, 3.64; F, 12.11; O, 13.60; S, 6.81
HS Tariff Code
2934.99.9001
Shipping
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.
Stock Solution Storage
0-4 °C for short term (days to weeks), or -20 °C for long term (months).