3048537-48-7
Chemical Structure
HPK1-IN-54
- CAS No.: 3048537-48-7
- Formula:C32H34FN7O3
- Molecular Weight:583.66
InChIKey: IXODLXIXCSDAQS-UHFFFAOYSA-N
SMILES: FC1=CC2=NC=C(N2C=C1)C3=C(CNC4=O)C4=C(NC5=CC=C(C67CCOCC7)C(CN6CCN8CCOCC8)=N5)C=C3
Biological Activity: HPK1-IN-54 is a potent HPK1 (Hematopoietic Progenitor Kinase 1) inhibitor that enhances T cell activation and proliferation by inhibiting HPK1 activity, thereby exhibiting antitumor effects. Its IC50 value against HPK1 is 2.67 nM, with excellent selectivity over the MAP4K family (>100-fold) and other selected kinases (>300-fold). HPK1-IN-54 displayed moderate in vivo clearance and reasonable oral exposure in mice and rats. Additionally, HPK1-IN-54 demonstrated strong antitumor efficacy in a CT26 murine colon cancer model and synergistic effects when combined with anti-PD-1 (HY-P9902A). HPK1-IN-54 shows promise for research in the field of immunotherapy[1].
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HPK1-IN-54 | HPK1-IN-54 is a potent HPK1 (Hematopoietic Progenitor Kinase 1) inhibitor that enhances T cell activation and proliferation by inhibiting HPK1 activity, thereby exhibiting antitumor effects. Its IC50 value against HPK1 is 2.67 nM, with excellent selectivity over the MAP4K family (>100-fold) and other selected kinases (>300-fold). HPK1-IN-54 displayed moderate in vivo clearance and reasonable oral exposure in mice and rats. Additionally, HPK1-IN-54 demonstrated strong antitumor efficacy in a CT26 murine colon cancer model and synergistic effects when combined with anti-PD-1 (HY-P9902A). HPK1-IN-54 shows promise for research in the field of immunotherapy. | |||||||||||||||||||||
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