LSZ102 | CAS#2135600-76-7 | SERD

LSZ102
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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.

Chemical Structure

LSZ102

CAS# 2135600-76-7

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 206950
Name: LSZ102
CAS#: 2135600-76-7
Chemical Formula: C25H17F3O4S
Exact Mass: 470.08
Molecular Weight: 470.462
Elemental Analysis: C, 63.83; H, 3.64; F, 12.11; O, 13.60; S, 6.81

Price and Availability

Size	Price	Availability
200mg	USD 3650	2 Weeks
500mg	USD 4950	2 Weeks
1g	USD 6950	2 Weeks
2g	USD 11950	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

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.

Product Data:

Product Data

Instruction:

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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

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	100.0	212.56

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
In vitro protocol:	TBD
In vivo protocol:	TBD

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

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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

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