A PROTAC that drives ER degradation
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ARV-471

Item No. 43002

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3S)-3-[1,3-dihydro-1-oxo-5-[4-[[1-[4-[(1R,2S)-1,2,3,4-tetrahydro-6-hydroxy-2-phenyl-1-naphthalenyl]phenyl]-4-piperidinyl]methyl]-1-piperazinyl]-2H-isoindol-2-yl]-2,6-piperidinedione
CAS Number
2229711-68-4
Synonyms
  • Vepdegestrant
Molecular Formula
C45H49N5O4
Formula Weight
723.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
H2O: Slightly soluble: 0.1-1 mg/ml
SMILES
OC1=CC=C2[C@@H](C3=CC=C(N(CC4)CCC4CN5CCN(C6=CC=C7C(CN([C@@H](CCC8=O)C(N8)=O)C7=O)=C6)CC5)C=C3)[C@@H](C9=CC=CC=C9)CCC2=C1
InChi Code
InChI=1S/C45H49N5O4/c51-37-12-15-39-33(27-37)8-13-38(31-4-2-1-3-5-31)43(39)32-6-9-35(10-7-32)48-20-18-30(19-21-48)28-47-22-24-49(25-23-47)36-11-14-40-34(26-36)29-50(45(40)54)41-16-17-42(52)46-44(41)53/h1-7,9-12,14-15,26-27,30,38,41,43,51H,8,13,16-25,28-29H2,(H,46,52,53)/t38-,41+,43+/m1/s1
InChi Key
TZZDVPMABRWKIZ-XMOGEVODSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $329

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    5 mg

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    10 mg

    $1,316

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    Cayman Chemical
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    Product Description

    ARV-471 is a proteolysis-targeting chimera (PROTAC) containing a derivative of the estrogen receptor (ER) modulator lasofoxifene conjugated to the immunomodulatory cereblon ligand lenalidomide (Item No. 14643).1 It induces degradation of ER in MCF-7 breast cancer cells with a half-maximal degradation concentration (DC50) value of 0.9 nM. ARV-471 also induces degradation of ER in cells expressing a variety of clinically relevant ER mutants. It inhibits the growth of T47D triple-negative breast cancer cells and MCF-7 cells expressing wild-type ER (GI50s = 4.5 and 3.3 nM, respectively) and T47D cells expressing ERY537S or ERD538G hormone-independent activating mutations (GI50s = 8 and 5.7 nM, respectively). ARV-471 (3, 10, and 30 mg/kg per day) reduces tumor growth in an MCF-7 orthotopic mouse xenograft model. It induces tumor regression in a patient-derived xenograft (PDX) ERY537S-expressing mouse model of breast cancer when administered at doses of 10 and 30 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gough, S.M., Flanagan, J.J., Teh, J., et al. Oral estrogen receptor PROTAC vepdegestrant (ARV-471) is highly efficacious as monotherapy and in combination with CDK4/6 or PI3K/mTOR pathway inhibitors in preclinical ER+ breast cancer models. Clin. Cancer Res. 30(16), 3549-3563 (2024).