BWA-522

CAT: 0804-HY-149433-01Size: 1 mgDry Ice: NoHazardous: No
CAT#:0804-HY-149433-01Size:1 mg
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Description
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].
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

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