PROTAC HER2 degrader-1

PROTAC HER2 degrader-1 is a highly selective HER2 PROTAC degrader, with a DC50 of 69 nM and a Dmax of 96%. PROTAC HER2 degrader-1 inhibits HER2-positive cell proliferation and tumor growth through persistent HER2 degradation and potent inhibition of downstream pathways (AKT and ERK) . PROTAC HER2 degrader-1 induces apoptosis in BT-474 cells. PROTAC HER2 degrader-1 can be used for research of HER2-positive cancers. (Pink: HER2 ligand: (HY-177009) ; Black: Linker; Blue: CRBN ligand: (HY-W023573) [1].

Product Specifications

CAS Number

[2897640-93-4]

UNSPSC

12352005

Target

Akt; Apoptosis; EGFR; ERK; PROTACs

Related Pathways

Apoptosis; JAK/STAT Signaling; MAPK/ERK Pathway; PI3K/Akt/mTOR; PROTAC; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Purity

98.0

Smiles

O=C1C2=CC=C(NCCCCCCCN3CCN(CCCOC4=CC5=NC=NC(NC6=CC=C(C(C)=C6)OC7=CC8=NC=NN8C=C7)=C5C=C4OC)CC3)C=C2C(N1C9C(NC(CC9)=O)=O)=O

Molecular Formula

C49H55N11O7

Molecular Weight

910.03

References & Citations

[1]Hu M, et al. Discovery of potent and selective HER2 PROTAC degrader based Tucatinib with improved efficacy against HER2 positive cancers. Eur J Med Chem. 2022 Dec 15;244:114775.