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KTX-582 is a potent IRAK4 degrader that can induce apoptosis in MYD88MT DLBCL and is efficient in inducing in vivo tumor regressions in a lymphoma model. It degrades IRAK4 in whole blood monocytes and lymphocytes with high potency.
Potent IRAK4 degrader with DC50 values of 4 nM for IRAK4 and 5 nM for Ikaros
Induces apoptosis in MYD88MT DLBCL
Efficient in inducing in vivo tumor regressions in a lymphoma model
Degrades IRAK4 in whole blood monocytes and lymphocytes with IC50s of less than 0.05 μM
Inhibits IRAK4 in human whole blood LPS TNFα with an IC50 of 0.05 to 1 μM
Exhibits antiproliferative activity against human OCI-Ly10 cells (IC50: 14 nM)
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