ERD-308, CAS 2320561-35-9

Formulation: A solid

Formal Name: (2S,4R)-1-((S)-2-(2-((5-(ethyl(2-(4-(6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thiophene-3-carbonyl)phenoxy)ethyl)amino)pentyl)oxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

Purity: ≥98%

Formula Markup: C55H65N5O9S2

CAS Number: 2320561-35-9

Notes: ERD-308 is a proteolysis-targeting chimera (PROTAC) containing the selective estrogen receptor modulator raloxifene (Item No. 10011620) conjugated to VHL ligand 1 (Item No. 21591).{67761} It induces degradation of estrogen receptor α (ERα) in MCF-7 and T47D breast cancer cells with half-maximal degradation concentration (DC50) values of 0.17 and 0.43 nM, respectively. ERD-308 inhibits the growth of MCF-7 cells (GI50 = 0.77 nM). It reduces the levels of mRNA encoding progesterone receptor and gene regulated in breast cancer 1 (GREB1) to an equivalent extent as the selective estrogen receptor degrader fulvestrant (Item No. 10011269) in MCF-7 cells when used at concentrations ranging from 1 to 300 nM.

• Artikelnummer: CAY33388-1
• Hersteller: Cayman Chemical
• Hersteller Artikelnummer: 33388-1
• Verpackungseinheit: 1 mg
• Mengeneinheit: STK