Potent and selective BTK Degrader (IC50 = 5.1 nM), degrades BTK in a proteasome- and CRBN-dependent manner. Suppresses BTK signaling and proliferation in mantle cell lymphoma (MCL) cells by degrading BTK, IKFZ1, and IKFZ3 (3 validated targets in B-cell malignancies). Also degrades Ibrutinib-resistant C481S-BTK mutant cancer cells. Exhibits no binding against a panel of 468 kinases at 1 µM. Reduces tumor burden and extends survival in lymphoma patient-derived xenograft models.
Molecular Weight:
991.163
CAS Number:
[2366132-45-6]
Formula:
C55H62N10O8
Target:
BTK|||Others|||PROTACs
T35481
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