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Chemical Structure : NX-5948
Catalog No.: PC-21323Not For Human Use, Lab Use Only.
NX‑5948 (NX5948) is a potent, selective and brain-penetrant degrader of BTK with DC50 of <1 nM in lymphoma cell lines and peripheral blood mononuclear cells (PBMCs).
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NX‑5948 (NX5948) is a potent, selective and brain-penetrant degrader of BTK with DC50 of <1 nM in lymphoma cell lines and peripheral blood mononuclear cells (PBMCs).
NX-5948 impairs viability in the BTK-dependent ABC-DLBCL cell line, TMD8 (EC 50: < 10 nM after 72 hours).
NX-5948 induces degradation of the mutated BTK-C481S in cells and inhibits proliferation of BTK-C481S mutant TMD8 cells more effectively than ibrutinib (NX-5948 EC 50 values of < 10 nM versus > 1 μM for ibrutinib).
NX-5948 demonstrates robust BTK degradation without significant downregulation of other off-target proteins.
NX-5948 demonstrates superior tumor growth inhibition (TGI) as compared to ibrutinib in TMD8 xenograft model in mice containing the BTK-C481S mutation.
NX-5948 penetrates the central nervous system (CNS) and demonstrates activity in a model of brain malignancies.
| M.Wt | 806.97 | |
| Formula | C42H54N12O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Daniel W Robbins, et al. Blood (2021) 138 (Supplement 1): 2251.
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