DD 03-171

CAT: 0931-MF-0051620Size: 5 mgDry Ice: NoHazardous: No
CAT#:0931-MF-0051620Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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CAS Number
2366132-45-6
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

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