A PROTAC that drives AR degradation
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ARD-2128

Item No. 40964

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[trans-3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]-4-[4-[[1-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-4-piperidinyl]methyl]-1-piperazinyl]-benzamide
CAS Number
2222111-87-5
Molecular Formula
C45H50ClN7O6
Formula Weight
820.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 1-10 mg/ml
SMILES
O=C(C1=CC=C(N2CCN(CC3CCN(C(C=C4C(N5C6CCC(NC6=O)=O)=O)=CC=C4C5=O)CC3)CC2)C=C1)N[C@@H]7C(C)([C@H](C(C)7C)OC8=CC(Cl)=C(C#N)C=C8)C
InChi Code
InChI=1S/C45H50ClN7O6/c1-44(2)42(45(3,4)43(44)59-32-11-7-29(25-47)35(46)24-32)49-38(55)28-5-8-30(9-6-28)52-21-19-50(20-22-52)26-27-15-17-51(18-16-27)31-10-12-33-34(23-31)41(58)53(40(33)57)36-13-14-37(54)48-39(36)56/h5-12,23-24,27,36,42-43H,13-22,26H2,1-4H3,(H,49,55)(H,48,54,56)/t36?,42-,43-
InChi Key
BWDWHHAZFQBJQL-JABICJEXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $142

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    5 mg

    $675

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    10 mg

    $1,065

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    25 mg

    $2,129

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    Cayman Chemical
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    Product Description

    ARD-2128 is a proteolysis targeting chimera (PROTAC) that is composed of an androgen receptor (AR) antagonist and thalidomide, a ligand for the E3 ubiquitin ligase cereblon.1 It induces degradation of ARs in VCaP and LNCaP prostate cancer cells with half-maximal degradation (DC50) concentrations of 0.3 and 8.3 nM, respectively, and inhibits the proliferation of VCaP and LNCaP cells (IC50s = 4 and 5 nM, respectively). ARD-2128 (10 mg/kg) decreases intratumoral protein levels of AR and the mRNA encoding puromycin-sensitive aminopeptidase (PSA), transmembrane serine protease 2 (TMPRSS2), and FK-506 binding protein 5 (FKBP5), but not mRNA encoding AR, in a VCaP mouse xenograft model. It reduces tumor volume in the same mice when administered at doses of 20 or 40 mg/kg per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Han, X., Zhao, L., Xiang, W., et al. Strategies toward discovery of potent and orally bioavailable proteolysis targeting chimera degraders of androgen receptor for the treatment of prostate cancer. J. Med. Chem. 64(17), 12831-12854 (2021).