For research use only. Not for therapeutic Use.
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].
| Catalog Number | I018969 |
| CAS Number | 2320561-35-9 |
| Synonyms | (2S,4R)-1-[(2S)-2-[[2-[5-[ethyl-[2-[4-[6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophene-3-carbonyl]phenoxy]ethyl]amino]pentoxy]acetyl]amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide |
| Molecular Formula | C55H65N5O9S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C55H65N5O9S2/c1-7-59(26-28-69-43-22-17-37(18-23-43)49(65)48-44-24-21-41(62)30-46(44)71-51(48)39-15-19-40(61)20-16-39)25-9-8-10-27-68-32-47(64)58-52(55(4,5)6)54(67)60-31-42(63)29-45(60)53(66)57-34(2)36-11-13-38(14-12-36)50-35(3)56-33-70-50/h11-24,30,33-34,42,45,52,61-63H,7-10,25-29,31-32H2,1-6H3,(H,57,66)(H,58,64)/t34-,42+,45-,52+/m0/s1 |
| InChIKey | BQXUPNKLZNSUMC-YUQWMIPFSA-N |
| SMILES | CCN(CCCCCOCC(=O)NC(C(=O)N1CC(CC1C(=O)NC(C)C2=CC=C(C=C2)C3=C(N=CS3)C)O)C(C)(C)C)CCOC4=CC=C(C=C4)C(=O)C5=C(SC6=C5C=CC(=C6)O)C7=CC=C(C=C7)O |
| Reference | [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. |
