3047066-15-6
Chemical Structure
DD205-291
- CAS No.: 3047066-15-6
- Formula:C38H38ClF3N10O3
- Molecular Weight:775.22
InChIKey: NQZCBDOOYGTFSB-UHFFFAOYSA-N
SMILES: O=C(N1)N(C2=C(C=CC(C(N3CCC(CC3)CC4CCN(CC4)C5=CC=C(C=N5)C6=NC7=C(NC=C7C8=CN(N=C8)CC(F)(F)F)N=C6)=O)=C2)Cl)CCC1=O
Biological Activity: DD205-291 is a selective, orally active HPK1 PROTAC degrader with a DC50 of 8.8 nM. By inducing complete degradation of HPK1 protein, DD205-291 simultaneously blocks both its kinase-dependent functions and non-kinase scaffold functions. DD205-291 inhibits the phosphorylation of SLP-76 with an EC50 of 22.98 nM. DD205-291 induces the production of IL-2 and IFN-γ with EC50 values of 34.68 nM and 32.6 nM, respectively. Combined with anti-PD1 in mouse models, DD205-291 exerts tumor-suppressive effects with favorable safety profiles. DD205-291 can be used in colon cancer-related research[1].
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DD205-291 | DD205-291 is a selective, orally active HPK1 PROTAC degrader with a DC50 of 8.8 nM. By inducing complete degradation of HPK1 protein, DD205-291 simultaneously blocks both its kinase-dependent functions and non-kinase scaffold functions. DD205-291 inhibits the phosphorylation of SLP-76 with an EC50 of 22.98 nM. DD205-291 induces the production of IL-2 and IFN-γ with EC50 values of 34.68 nM and 32.6 nM, respectively. Combined with anti-PD1 in mouse models, DD205-291 exerts tumor-suppressive effects with favorable safety profiles. DD205-291 can be used in colon cancer-related research. | |||||||||||||||||||||
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Keywords
