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ER degrader 5

CAS: 2913192-47-7 F: C26H18F2O4S W: 464.48

ER degrader 5 is a potent estrogen receptor (ER) degrader. ER degrader 5 shows anti-proliferation activity. ER degrader
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Bioactivity ER degrader 5 is a potent estrogen receptor (ER) degrader. ER degrader 5 shows anti-proliferation activity. ER degrader 5 can be used for the research of breast cancer[1].
Invitro ER degrader 5 (compound 27d) (5 days) 抑制 MCF-7 细胞的增殖,IC50 值为 55 nM[1]。ER degrader 5 阻断 MCF-7 细胞 G0/G1 期细胞周期[1]。ER degrader 5 (1 nM-10 μM; 24 h) 降解 MCF-7 细胞中的雌激素受体 (ER)[1]。ER degrader 5 (1-10 μM; 24 h) 显着降低 MCF-7 细胞中GREB1,PGR 和 TFF1 的表达水平[1]。 Western Blot Analysis[1] Cell Line:
In Vivo ER degrader 5 (compound 27d) (30 mg/kg; i.p. daily for 30 days) 显着抑制 MCF-7 异种移植模型中的肿瘤生长[1]。ER degrader 5 (3 mg/kg; i.v.) 的半衰期为 1.23 小时,Cmax 为 4497 ng/mL[1]。ER degrader 5 (30 mg/kg; p.o.) 产生 62.9% 的口服生物利用度[1]。 Animal Model:
Name ER degrader 5
CAS 2913192-47-7
Formula C26H18F2O4S
Molar Mass 464.48
Transport Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Reference [1]. Lu Y, et, al. Design, synthesis and biological evaluation of fluorinated selective estrogen receptor degraders (FSERDs) --- A promising strategy for advanced ER positive breast cancer. Eur J Med Chem. 2023 May 5;253:115324.