ERD-308

• CAS: 2320561-35-9
• Catalog Number: ACM2320561359
• Category: Others
• Molecular Weight: 1004.27
• Molecular Formula: C55H65N5O9S2
• Description: ERD-308 is a Highly Potent Proteolysis Targeting Chimera Degrader of Estrogen Receptor (ER) 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.
• Synonyms: ERD-308; ERD 308; ERD308
• IUPAC Name: (2S,4R)-1-((S)-2-(2-((5- (Ethyl(2-(4-(6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thiophene-3-carbonyl)phenoxy)ethyl)-amino)pentyl)oxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide
• Canonical SMILES: O=C([C@H]1N(C([C@@H](NC(COCCCCCN(CC)CCOC2=CC=C(C(C3=C(C4=CC=C(O)C=C4)SC5=CC(O)=CC=C53)=O)C=C2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C
• 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
• InChI Key: BQXUPNKLZNSUMC-YUQWMIPFSA-N
• Solubility: Soluble in DMSO
• Appearance: Solid powder
• Shelf Life: >3 years if stored properly
• Storage: Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
• Drug Formulation: This drug may be formulated in DMSO
• Elemental Analysis: C, 65.78; H, 6.52; N, 6.97; O, 14.34; S, 6.38
• Exact Mass: 1003.4224
• HS Tariff Code: 2934.99.9001
• In Vitro Activity: 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.; Reference: J Med Chem. 2019 Feb 14;62(3):1420-1442. https://pubmed.ncbi.nlm.nih.gov/30990042/
• In Vivo Activity: TBD
• Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).