Description
ERα degrader 10 is a selective and orally active estrogen receptor α (ERα) degrader. ERα degrader 10 exhibits potent ERα binding affinity (IC50 of 24.0 nM) and degradation ability (EC50 of 5.3 nM). ERα degrader 10 degrades ERα through the proteasome-mediated pathway. ERα degrader 10 can be used for the study of breast cancer.
Product information
Molecular Weight: 468.97
Formula: C29H25ClN2O2
Smiles: CC/C(=C(\C1C=CC(=CC=1)C1=CN(C)N=C1)/C1C=CC(/C=C/C(O)=O)=CC=1)/C1=CC=CC=C1Cl
InChiKey: YSADBXRMBYOBNA-UNOKIKLSSA-N
InChi: InChI=1S/C29H25ClN2O2/c1-3-25(26-6-4-5-7-27(26)30)29(22-11-8-20(9-12-22)10-17-28(33)34)23-15-13-21(14-16-23)24-18-31-32(2)19-24/h4-19H,3H2,1-2H3,(H,33,34)/b17-10+,29-25+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: To be determined
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
ERα degrader 10 (Compound A20) shows outstanding anti-proliferative effects on MCF-7 cells (IC50 = 0.28 nM). ERα degrader 10 (Compound A20; 0.1-1000 nM; 1-48 h) shows the ERα degradation in a concentration-dependent manner, and the degradation effect is best at 24 h via a proteasome-mediated protein degradation pathway[1]. ERα degrader 10 (10-100 nM; 24 h) could suppress the ERα signal transduction, inducing the MCF-7 cell cycle arrest in G1 phase.
In Vivo:
ERα degrader 10 (10-30 mg/kg; po; daily; for 30 days) shows excellent antitumor effect in the MCF-7 xenograft model in vivo.
Products are for research use only. Not for human use.
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