| Chemical Properties | Back Directory | [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) | [form ]
Solid | [pka]
8.83±0.15(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [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_
_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. | [storage]
4°C, protect from light | [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 |
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| Company Name: |
Wuhan Topule
|
| Tel: |
+86-02787215551 +86-19945035818 |
| Website: |
http://www.topule.com/ |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|