DD 03-171 - CAS 2366132-45-6

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.

PROTACs, Others, BTK

PROTAC, Tyrosine Kinase/Adaptors, Others, Angiogenesis

2366081

C55H62N10O8

991.163

Cc1c(NC(=O)c2ccc(cc2)C(C)(C)C)cccc1-c1cn(C)c(=O)c(Nc2ccc(cc2)C(=O)N2CCN(CCCCCCNC(=O)CNc3cccc4C(=O)N(C5CCC(=O)NC5=O)C(=O)c34)CC2)n1

-20°C

Ice Packs

Small Compound