ERα degrader-2

Research use only, not for human use.

ERα degrader-2 is a selective and potent estrogen receptor (SERD) degrader with anticancer activity, exhibiting an EC50 value of 0.3 nM for ERα degradation.

ERα degrader-2 is a selective estrogen receptor degrader (SERD) with potent binding affinity with ERα (IC50=17.1 nM), good degradation efficacy (EC50=0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent agentgability, can be used for HER+ breast cancer research.

ERα degrader-2 (0.01-40 nM) decreases ERα expression and not fully degrades ERα in MCF-7 cells even at a higher biochemical concentration in MCF7 cells.

ERα degrader-2 (oral administration; 2-6 mg/kg; QD; 21 days)leads to the significant tumor growth inhibition and decreases tumor volume in mice.ERα degrader-2 (oral gavage; 2 mg/kg; single dose) possesses better pharmacokinetic properties than?AZD9496, the plasma exposure (AUC) is 16073.7 h*ng/mL, and the half-life period is 12.1 h, the oral availability is 80.5%.Animal Model:MCF-7 human breast cancer xenograft model in nude mice Dosage:2 mg/kg; 6 mg/kg Administration:Oral administration; 2-6 mg/kg; QD; 21 days Result:Exhibited in vivo efficacy in breast cancer xenograft model.

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MAPK/ERK Signaling

ERK

ERK

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2235396-63-9

492.53

C29H27F3N2O2

>98% (HPLC)

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[H][C@@]1(N(CC(C)(C)F)[C@H](C)Cc2c1[nH]c1ccccc21)c1c(F)cc(cc1F)-c1ccc(cc1)C(O)=O

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(-20℃)

With Ice Pack

≥ 2 years