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BWA-522

BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7. BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor (Androgen Receptor) and induces apoptosis in PC cells. BWA-522 inhibits tumor growth in LNCaP xenograft model studies (60 mg/kg, po; TGI=76%) . The efficiencies of BWA-522 in degrading AR-V7 and AR-FL were 77.3% (1 μM) and 72.0% (5 μM) in VCaP and LNCaP cells, respectively[1].

Product Specifications

CAS Number

[3042820-12-9]

UNSPSC

12352005

Target

Androgen Receptor; Apoptosis

Type

Reference compound

Related Pathways

Apoptosis; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/bwa-522.html

Concentration

10mM

Purity

99.93

Solubility

DMSO : 90 mg/mL (ultrasonic)

Smiles

CC(C1=CC=C(OC[C@H](O)CCl)C=C1)(C)C(C=C2)=CC=C2OCC3CCN(CC4CCN(C5=CC=C6C(C(N(C7CCC(NC7=O)=O)C6=O)=O)=C5)CC4)CC3

Molecular Formula

C43H51ClN4O7

Molecular Weight

771.34

References & Citations

[1]Zhang B, et al. Discovery of BWA-522, a First-in-Class and Orally Bioavailable PROTAC Degrader of the Androgen Receptor Targeting N-Terminal Domain for the Treatment of Prostate Cancer. J Med Chem. 2023 Aug 24;66 (16) :11158-11186..

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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