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PROTAC AR Degrader-12

CAT: 0804-HY-179433Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-179433Size:1 Each
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS) . PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer[1].
UNSPSC
12352005
Target
Androgen Receptor; Estrogen Receptor/ERR; PROTACs; Src
Related Pathways
PROTAC; Protein Tyrosine Kinase/RTK; Vitamin D Related/Nuclear Receptor
Field of Research
Cancer
Smiles
CC(COC1=C(C=CC(C(N2CCC(CN3CCCC(C(N[C@@H](C(C)(C)C)C(N4[C@H](C(N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C)=O)C[C@@H](O)C4)=O)=O)C3)CC2)=O)=C1)NC(C7=CC(OCC(C)C)=C(C=C7)[N+]([O-])=O)=O)C
Molecular Formula
C57H76N8O10S
Molecular Weight
1065.33
References & Citations
[1]Wu Y, et al. Kill Two Birds with One Stone: An Efficient and Potent AR CBS-Targeted Degrader Reverses Breast Cancer Resistance via Concurrent AR Degradation and ERα Transcriptional Suppression. J Med Chem. 2025 Nov 27;68 (22) :24136-24167.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
ERα

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