| CAS NO: | 2135600-76-7 |
| 包装 | 价格(元) |
| 25mg | 电议 |
| 5mg | 电议 |
| Cas No. | 2135600-76-7 |
| 化学名 | (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 |
| 分子式 | C25H17F3O4S |
| 分子量 | 470.46 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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. |
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