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| | ERD-308 Basic information |
| Product Name: | ERD-308 | | Synonyms: | ERD-308;(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;CID 138454799 | | CAS: | 2320561-35-9 | | MF: | C55H65N5O9S2 | | MW: | 1004.27 | | EINECS: | | | Product Categories: | | | Mol File: | 2320561-35-9.mol |  |
| | ERD-308 Chemical Properties |
| 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 |
| | ERD-308 Usage And Synthesis |
| 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. | | Uses | ERD-308 is a highly potent von Hippel-Lindau-based PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment. ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM in both cell lines (DC50 (concentration causing 50% of protein degradation) of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells, respectively)[1]. | | 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_
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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. | | References | [1] Hu J, et al. Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER). J Med Chem. 2019 Feb 14;62(3):1420-1442. DOI:10.1021/acs.jmedchem.8b01572 |
| | ERD-308 Preparation Products And Raw materials |
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