LSZ102 |
| Catalog No.GC18155 |
Estrogen receptor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2135600-76-7
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
LSZ102 exhibit oral bioavailability and preclinical activity as selective estrogen receptor degraders (SERDs). It is a compound in clinical development for the treatment of ERα positive breast cancer.
In Phase I/Ib trials for the treatment of ERα positive breast cancer, LSZ-102 has an IC50 of 0.2 nM. LSZ-102 induces significant degradation of ERα after 24 h, when given as a 10 μM solution to MCF-7 cells.
Treatment of the mice with LSZ102 once daily at 20 mg/kg resulted in significant tumor growth inhibition as compared to the control group treated with vehicle alone, resulting in tumor stasis (mean change in tumor volume of LSZ102 vs control = %ΔT/ΔC of 2.4% on day 48, p < 0.05).
Dosing of 3 mg/kg solution of LSZ102 in male Sprague−Dawley rats resulted in 33% bioavailability and a dose-normalized exposure of 620 nM·h
References
1. Tria GS, et al. Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer. J Med Chem. 2018 Apr 12;61(7):2837-2864.
| Cas No. | 2135600-76-7 | SDF | |
| Chemical Name | (E)-3-(4-((2-(2-(1,1-difluoroethyl)-4-fluorophenyl)-6-hydroxybenzo[b]thiophen-3-yl)oxy)phenyl)acrylic | ||
| Canonical SMILES | OC(/C=C/C1=CC=C(OC2=C(C3=C(C(F)(F)C)C=C(F)C=C3)SC4=C2C=CC(O)=C4)C=C1)=O | ||
| Formula | C25H17F3O4S | M.Wt | 470.46 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1256 mL | 10.6279 mL | 21.2558 mL |
| 5 mM | 0.4251 mL | 2.1256 mL | 4.2512 mL |
| 10 mM | 0.2126 mL | 1.0628 mL | 2.1256 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *