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PROTAC AR Degrader-8

PROTAC AR Degrader-8 (Compound NP18) is the PROTAC degrader for androgen receptor (AR), that degrades AR-FL with DC50 of 0.018 μM and 0.14 μM in 22Rv1 cell and LNCaP cell, degrades AR-V7 with DC50 of 0.026 μM in 22Rv1 cell. PROTAC AR Degrader-8 inhibits the proliferation of cancer cell 22Rv1 and LNCaP with IC50 of 0.038 μM and 1.11 μM. PROTAC AR Degrader-8 arrests cell cycle at G2/M phase, induces apoptosis in 22Rv1 cell. PROTAC AR Degrader-8 exhibits anticancer efficacy in mouse and zebrafish model[1]. (Pink: ligand for target protein AR ligand-33 (HY-170330) ; Black: linker (HY-W007731) ; Blue: ligand for E3 ligase Cereblon (HY-14658) )

Product Specifications

CAS Number

[3044108-04-2]

UNSPSC

12352005

Target

Androgen Receptor; Apoptosis; PROTACs

Related Pathways

Apoptosis; PROTAC; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Purity

99.98

Solubility

DMSO : ≥ 100 mg/mL

Smiles

O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3NCCOC4=CC=C(C(C)(C5=CC=C(OCC6=NC(N7CCOCC7)=CC=C6)C=C5)C)C=C4)=O

Molecular Formula

C40H41N5O7

Molecular Weight

703.78

References & Citations

[1]Ha S, et al., Discovery of a highly potent, N-terminal domain-targeting degrader of AR-FL/AR-V7 for the treatment of prostate cancer. Eur J Med Chem. 2025 Jan 15;282:117079.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Available Sizes

Curated Selection

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