ERD-308
- Product Name
- ERD-308
- CAS No.
- 2320561-35-9
- Chemical Name
- ERD-308
- Synonyms
- ERD-308;CID 138454799;(2S,4R)-1-[(2S)-2-[2-({5-[ethyl(2-{4-[6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophene-3-carbonyl]phenoxy}ethyl)amino]pentyl}oxy)acetamido]-3,3-dimethylbutanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide
- CBNumber
- CB38054589
- Molecular Formula
- C55H65N5O9S2
- Formula Weight
- 1004.27
- MOL File
- 2320561-35-9.mol
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
N-Bromosuccinimide Price
- Product number
- 027684
- Product name
- ERD-308
- Packaging
- 001
- Price
- $1300
- Updated
- 2021/12/16
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.
ERD-308 Preparation Products And Raw materials
Raw materials
Preparation Products
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