A potent and covalent BTK inhibitor (IC50 = 0.3 nM); selective for BTK over a panel of 304 kinases at 1 μM; inhibits EGFR

Zanubrutinib – 25 mg

Brand:
Cayman
CAS:
1691249-45-2
Storage:
-20
UN-No:
Non-Hazardous - /

Zanubrutinib is a potent and covalent inhibitor of Bruton’s tyrosine kinase (BTK; IC50 = 0.3 nM).{52108} It is selective for BTK over a panel of 304 kinases at 1 μM but does inhibit EGFR, Tec, Blk, BMX, HER4, and TXK (IC50s = 0.62-33 nM). Zanubrutinib inhibits phosphorylation of BTK at Y233 (IC50 = 1.8 nM) in Ramos cells and reduces viability of REC-1 cells (IC50 = 0.36 nM). In vivo, zanubrutinib (2.5 and 7.5 mg/kg) reduces tumor volume in an OCI-LY10 diffuse large B cell lymphoma (DLBCL) mouse xenograft model.  

 

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SKU: 28924 - 25 mg Category:

Description

A potent and covalent BTK inhibitor (IC50 = 0.3 nM); selective for BTK over a panel of 304 kinases at 1 μM; inhibits EGFR, Tec, Blk, BMX, HER4, and TXK (IC50s = 0.62-33 nM); inhibits phosphorylation of BTK at Y233 (IC50 = 1.8 nM) in Ramos cells; reduces viability of REC-1 cells (IC50 = 0.36 nM); reduces tumor volume in an OCI-LY10 DLBCL mouse xenograft model at 2.5 and 7.5 mg/kg

Formal name: (7S)-4,5,6,7-tetrahydro-7-[1-(1-oxo-2-propen-1-yl)-4-piperidinyl]-2-(4-phenoxyphenyl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide

Synonyms:  BGB-3111

Molecular weight: 471.6

CAS: 1691249-45-2

Purity: ≥98%

Formulation: A solid

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