| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg | |||
| 50mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
Estrogen receptor (ER). ERD-308 is a highly potent PROTAC degrader of estrogen receptor (ER), utilizing the von Hippel-Lindau (VHL) E3 ligase for targeted protein degradation. It specifically degrades ER in ER-positive breast cancer cells.
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|---|---|
| ln Vitro |
ERD-308 induces potent ER degradation in MCF-7 and T47D ER+ cells with DC₅0 values of 0.17 nM and 0.43 nM, respectively. It induces >95% ER degradation at concentrations as low as 5 nM. The compound exhibits high potency in ER-positive breast cancer cell lines, reducing tumor cell proliferation.
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| ln Vivo |
In vivo, ERD-308 would be expected to demonstrate antitumor efficacy in ER-positive breast cancer xenograft models. By degrading ER, the compound blocks estrogen-driven tumor growth and overcomes resistance to endocrine therapies. Efficacy would be assessed by tumor growth inhibition, ER degradation in tumor tissues, and survival extension.
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| Enzyme Assay |
ER degradation assays are performed in ER-positive breast cancer cell lines (MCF-7, T47D). Cells are treated with serial dilutions of ERD-308 for 4-24 hours. ER protein levels are quantified by Western blotting or ELISA. DC₅0 values (concentration causing 50% protein degradation) are calculated from dose-response curves.
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| Cell Assay |
ER-positive breast cancer cell lines (MCF-7, T47D) are treated with ERD-308 at various concentrations. ER degradation is assessed by Western blotting. Cell viability is assessed using MTT or CellTiter-Glo assays. Estrogen-responsive gene expression (e.g., pS2, GREB1) is measured by qPCR. Apoptosis and cell cycle changes are evaluated by flow cytometry.
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| Animal Protocol |
Mice bearing subcutaneous ER-positive breast cancer xenografts (MCF-7 or T47D) are administered ERD-308 via intraperitoneal or intravenous injection. Tumor growth is monitored by caliper measurements. Tumors are harvested for pharmacodynamic analysis of ER degradation, estrogen-responsive gene expression, and apoptosis markers. Efficacy is determined by tumor growth inhibition.
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| ADME/Pharmacokinetics |
ERD-308 has a molecular weight of 1004.26 g/mol and formula C₅₅H₆₅N₅O₉S2. As a PROTAC molecule, it may have limited oral bioavailability and is typically administered parenterally. Standard PK parameters would be determined in rodent studies following IV administration.
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| Toxicity/Toxicokinetics |
Toxicology data for ERD-308 are not publicly available. Standard preclinical safety assessment would include cytotoxicity screening, hERG testing, and repeat-dose toxicology studies in rodents. Given the role of ER in normal physiology, potential on-target toxicities (e.g., endocrine effects) would be evaluated.
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| References | |
| Additional Infomation |
ERD-308 is a research compound for ER-positive breast cancer studies. It is not clinically approved. ERD-308 is a highly potent VHL-based PROTAC degrader that provides a tool for studying ER signaling, resistance mechanisms, and targeted protein degradation as a therapeutic strategy for hormone-driven cancers.
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| Molecular Formula |
C55H65N5O9S2
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|---|---|
| Molecular Weight |
1004.26271224022
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| Exact Mass |
1003.42
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| Elemental Analysis |
C, 65.78; H, 6.52; N, 6.97; O, 14.34; S, 6.38
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| CAS # |
2320561-35-9
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| PubChem CID |
138454799
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| Appearance |
White to yellow solid powder
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| LogP |
9
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
23
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| Heavy Atom Count |
71
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| Complexity |
1700
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CCN(CCCCCOCC(=O)N[C@H](C(=O)N1C[C@@H](C[C@H]1C(=O)N[C@@H](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
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| InChi Key |
BQXUPNKLZNSUMC-YUQWMIPFSA-N
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| InChi Code |
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
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| Chemical 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
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| Synonyms |
ERD308 ERD 308 ERD-308
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~49.79 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1.25 mg/mL (1.24 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1.25 mg/mL (1.24 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 1.25 mg/mL (1.24 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9958 mL | 4.9788 mL | 9.9576 mL | |
| 5 mM | 0.1992 mL | 0.9958 mL | 1.9915 mL | |
| 10 mM | 0.0996 mL | 0.4979 mL | 0.9958 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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