ERD-308 Property

Boiling point:

1173.0±65.0 °C(Predicted)

Density 

1.271±0.06 g/cm3(Predicted)

storage temp. 

4°C, protect from light

solubility 

DMSO:50.0(Max Conc. mg/mL);49.79(Max Conc. mM)

pka

8.83±0.15(Predicted)

form 

Solid

color 

White to yellow

Hazard and Precautionary Statements (GHS)

ERD-308 Chemical Properties,Usage,Production

Description

ERD-308 is a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER) ERD-308 achieves DC50_x000D_ (concentration causing 50% of protein degradation) values of 0.17 and 0.43 nM in MCF-7 and T47D ER+ breast cancer cell lines, respectively, and induces >95% of ER degradation at concentrations as low as 5 nM in both cell lines. Significantly, ERD-308 induces more complete ER degradation than fulvestrant, the only approved selective ER degrader (SERD), and is more effective in inhibition of cell proliferation than fulvestrant in MCF-7 cells.

in vitro

ERD-308 achieves DC50 (concentration causing 50% of protein degradation) values of 0.17 and 0.43 nM in MCF-7 and T47D ER+ breast cancer cell lines, respectively, and induces >95% of ER degradation at concentrations as low as 5 nM in both cell lines. Significantly, ERD-308 induces more complete ER degradation than fulvestrant, the only approved selective ER degrader (SERD), and is more effective in inhibition of cell proliferation than fulvestrant in MCF-7 cells._x000D_ _x000D_ Reference: J Med Chem. 2019 Feb 14;62(3):1420-1442. https://pubmed.ncbi.nlm.nih.gov/30990042/

target

ERD-308 is a highly potent PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment.