DD 03-171

• Target:

  PROTACs|||Others|||BTK

• Related Pathways:

  PROTAC|||Tyrosine Kinase/Adaptors|||Others|||Angiogenesis

• Bioactivity:

  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 ?M. Reduces tumor burden and extends survival in lymphoma patient-derived xenograft models.

• Smiles:

  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

• Molecular Formula:

  C55H62N10O8

• Molecular Weight:

  991.163

• Shipping Conditions:

  Cool pack

• Storage Temperature:

  -20°C

• CAS Number:

  2366132-45-6