LYA914
LYA914 is an orally active AR/AR-V7 PROTAC degrader. LYA914 targets the proteolytic degradation of the conserved DNA binding domain (DBD) of the androgen receptor (AR) . LYA914 exhibits potent antiproliferative effects in Enzalutamide (HY-70002) -insensitive/resistant cells. LYA914 inhibits tumor growth in VCaP/LNCaP tumor mouse models. LYA914 can be used to study castration-resistant prostate cancer (CRPC) . (Pink: AR-DBD ligand-1: HY-175456, Blue: Thalidomide: HY-14658, Pink + Black: AR-DBD ligand-Linker Conjugate 1: HY-175457, Black: Boc-piperidine-oxopiperidin: HY-175458) [1].
Product Specifications
UNSPSC
12352005
Target
Akt; Androgen Receptor; PROTACs
Related Pathways
PI3K/Akt/mTOR; PROTAC; Vitamin D Related/Nuclear Receptor
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Smiles
O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC(N4CCC(CN5CCC(N6CCN(C7=NC(C8=CC=C(F)C(F)=C8OC)=CS7)CC6)CC5)CC4)=C3)=O
Molecular Formula
C38H43F2N7O5S
Molecular Weight
747.85
References & Citations
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Cereblon
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KCNK1, CT (KCNK1, HOHO1, KCNO1, TWIK1, Potassium channel subfamily K member 1, Inward rectifying potassium channel protein TWIK-1, Potassium channel KCNO1) (Azide free) (HRP)