3108744-13-1
Chemical Structure
PROTAC HPK1 Degrader-5
- CAS No.: 3108744-13-1
- Formula:C43H45N11O5
- Molecular Weight:795.89
IUPAC Name: 3-((4-(1-(((3S)-1-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)pyrrolidin-3-yl)methyl)piperidin-4-yl)phenyl)amino)-6-(1-methyl-1H-benzo[d]imidazol-4-yl)-5-(methylamino)pyrazine-2-carboxamide
InChIKey: HBTZLNWFXFMHRZ-PPVAYSNCSA-N
SMILES: O=C(N)C1=NC(C2=C(C3=CC=C2)N=CN3C)=C(N=C1NC4=CC=C(C=C4)C5CCN(CC5)C[C@@H]6CCN(C6)C7=CC8=C(C=C7)C(N(C8=O)C9CCC(NC9=O)=O)=O)NC
Biological Activity: PROTAC HPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader (DC50 = 5.0 nM; Dmax ≥ 99%). PROTAC HPK1 Degrader-5 significantly inhibits SLP76 phosphorylation and enhanced ERK pathway activation through degrading HPK1, thereby stimulating IL-2 and IFN-γ release. PROTAC HPK1 Degrader-5 exhibits the ability to overcome the immunosuppressive effects imposed by PGE2, NECA or TGF-β. PROTAC HPK1 Degrader-5 alone efficaciously inhibits tumor growth in an MC38 syngeneic mouse model. PROTAC HPK1 Degrader-5 can be used for the study of tumor (such as colorectal cancer) immunotherapy[1].
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PROTAC HPK1 Degrader-5 | PROTAC HPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader (DC50 = 5.0 nM; Dmax ≥ 99%). PROTAC HPK1 Degrader-5 significantly inhibits SLP76 phosphorylation and enhanced ERK pathway activation through degrading HPK1, thereby stimulating IL-2 and IFN-γ release. PROTAC HPK1 Degrader-5 exhibits the ability to overcome the immunosuppressive effects imposed by PGE2, NECA or TGF-β. PROTAC HPK1 Degrader-5 alone efficaciously inhibits tumor growth in an MC38 syngeneic mouse model. PROTAC HPK1 Degrader-5 can be used for the study of tumor (such as colorectal cancer) immunotherapy. | |||||||||||||||||||||
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Keywords
