A PROTAC that drives ER degradation
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ERD-308

Item No. 33388

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal 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
CAS Number
2320561-35-9
Molecular Formula
C55H65N5O9S2
Formula Weight
1004.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlMethanol: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(C1=CC=C(C=C1)OCCN(CC)CCCCCOCC(N[C@@H](C(C)(C)C)C(N2[C@@H](C[C@H](C2)O)C(N[C@H](C3=CC=C(C4=C(C)N=CS4)C=C3)C)=O)=O)=O)C5=C(C6=CC=C(C=C6)O)SC7=CC(O)=CC=C75
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
InChi Key
BQXUPNKLZNSUMC-YUQWMIPFSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    500 µg

    $53

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    1 mg

    $101

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    Cayman Chemical
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    Product Description

    ERD-308 is a proteolysis-targeting chimera (PROTAC) containing the selective estrogen receptor modulator raloxifene (Item No. 10011620) conjugated to VHL ligand 1 (Item No. 21591).1 It induces degradation of estrogen receptor α (ERα) in MCF-7 and T47D breast cancer cells with half-maximal degradation concentration (DC50) values of 0.17 and 0.43 nM, respectively. ERD-308 inhibits the growth of MCF-7 cells (GI50 = 0.77 nM). It reduces the levels of mRNA encoding progesterone receptor and gene regulated in breast cancer 1 (GREB1) to an equivalent extent as the selective estrogen receptor degrader fulvestrant (Item No. 10011269) in MCF-7 cells when used at concentrations ranging from 1 to 300 nM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hu, J., Hu, B., Wang, M., et al. Discovery of ERD-308 as a highly potent proteolysis targeting chimera (PROTAC) degrader of estrogen receptor (ER). J. Med. Chem. 62(3), 1420-1442 (2019).