NX-5948 | BTK PROTAC | Probechem Biochemicals

Chemical Structure : NX-5948

CAS No.: 2649400-34-8

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NX-5948 (NX5948, Nx-5948)

货号: 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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1 mg	￥3580	In stock
5 mg	￥6580	In stock
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25 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	806.97
分子式	C42H54N12O5
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	3-((4-(1-((1-(6-(((S)-2,6-dioxopiperidin-3-yl)carbamoyl)pyridin-3-yl)piperidin-4-yl)methyl)piperidin-4-yl)phenyl)amino)-5-((R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl)pyrazine-2-carboxamide

参考文献

1. Daniel W Robbins, et al. Blood (2021) 138 (Supplement 1): 2251.

NX-5948 (NX5948, Nx-5948)

生物&药学活性

物理化学性质&存储条件

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NX-5948 (NX5948, Nx-5948)

生物&药学活性

物理化学性质&存储条件

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