PROTAC PI3Kα degrader-1
PROTAC PI3Kα degrader-1 is a PI3Kα PROTAC degrader (DC50 = 0.08 μM), demonstrating good selectivity for PI3Kα degradation over PI3Kβ, PI3Kγ, and PI3Kδ. PROTAC PI3Kα degrader-1 effectively degrades PI3Kα in a time- and concentration-dependent, over PI3Kβ, PI3Ky and PI3Kδ, and potently inhibited the phosphorylation of AKT at the Ser473site. PROTAC PI3Kα degrader-1 shows significant in vivo anticancer efficacy in HGC-27 and DOHH2 xenograft models. (Pink: PI3Kα ligand : (HY-174798), Blue: E3 ligase CRBN Ligand (HY-10984), Black: Linker, E3 ligase ligand-linker conjugate (HY-W940885) ) [1].
Product Specifications
UNSPSC
12352005
Target
PI3K; PROTACs
Related Pathways
PI3K/Akt/mTOR; PROTAC
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Smiles
O=S(NC1=C(N=CC(C2=CC3=C(N=CN=C3C(OCCCCCCCCCCCCNC4=CC=CC(C(N5C6CCC(NC6=O)=O)=O)=C4C5=O)=C2)C)=C1)OC)(C7=CC=C(C=C7F)F)=O
Molecular Formula
C46H49F2N7O8S
Molecular Weight
897.99
References & Citations
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Cereblon; PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ
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