3135155-78-8
Chemical Structure
PROTAC AURKA degrader-4
- CAS No.: 3135155-78-8
- Formula:C48H48ClN7O8S
- Molecular Weight:918.45
InChIKey: UBJKZMXTCSMSFS-UHFFFAOYSA-N
SMILES: CC1=C(C=C(C2=C1NC=C2)C3=CC=C(C(OC4=NC=CC=C4)=C3)Cl)C(NS(=O)(N5CCN(CC5)C(CCCCCCCC#CC6=CC=C7C(CN(C7=O)C8CCC(NC8=O)=O)=C6)=O)=O)=O
Biological Activity: PROTAC AURKA degrader-4 is a AURKA PROTAC degrader with a DC50 of 25.62 nM (Jurkat cells). PROTAC AURKA degrader-4 recruits the CRBN E3 ubiquitin ligase via the ubiquitin-proteasome system. PROTAC AURKA degrader-4 disrupts both the catalytic and non-catalytic functions of AURKA, including its interactions with TPX2 and c-Myc. PROTAC AURKA degrader-4 induces G2/M phase arrest and apoptosis. PROTAC AURKA degrader-4 exhibits enhanced antiproliferative activity and in vivo antitumor efficacy in models with high CRBN and AURKA expression. PROTAC AURKA degrader-4 can be used for the research of acute lymphoblastic leukemia[1].
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PROTAC AURKA degrader-4 | PROTAC AURKA degrader-4 is a AURKA PROTAC degrader with a DC50 of 25.62 nM (Jurkat cells). PROTAC AURKA degrader-4 recruits the CRBN E3 ubiquitin ligase via the ubiquitin-proteasome system. PROTAC AURKA degrader-4 disrupts both the catalytic and non-catalytic functions of AURKA, including its interactions with TPX2 and c-Myc. PROTAC AURKA degrader-4 induces G2/M phase arrest and apoptosis. PROTAC AURKA degrader-4 exhibits enhanced antiproliferative activity and in vivo antitumor efficacy in models with high CRBN and AURKA expression. PROTAC AURKA degrader-4 can be used for the research of acute lymphoblastic leukemia. | |||||||||||||||||||||
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