Zanubrutinib is a potent and specific irreversible BTK inhibitor with only weak off-target inhibitory effects on other kinases such as ITK, JAK3 and EGFR.

 

Brand: BCM

 

Target: BTK

 

Signaling Pathways: Angiogenesis; Tyrosine Kinase/Adaptors

 

In Vitro: In both biochemical and cellular assays, BGB-3111 demonstrated nanomolar BTK inhibition activity. In several MCL and DLBCL cell lines, BGB-3111 inhibited BCR aggregation-triggered BTK autophosphorylation, blocked downstream PLC-γ2 signaling, and potently inhibited cell proliferation. In comparison with ibrutinib, BGB-3111 showed much more restricted off-target activities against a panel of kinases, including ITK. While ibrutinib significantly inhibited rituximab-induced NK cell IFN-γ secretion and in vitro cytotoxicity on mantle cell lymphoma cells, BGB-3111 was at least 10-fold weaker than ibrutinib in inhibiting rituximab induced ADCC, consistent with its weak ITK inhibition activity. 

 

Boiling Point: 713.4±60.0 °C(Predicted)

 

pKa: 15.35±0.40(Predicted)

 

Solubility: Soluble in DMSO; Soluble in Ethanol. Insoluble in Water.

 

GHS: GHS07

 

Isomeric SMILES: C=CC(=O)N1CCC(CC1)[C@@H]2CCNC3=C(C(=NN23)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=O)N  

 

InChIKey: RNOAOAWBMHREKO-QFIPXVFZSA-N  

 

InChI: InChI=1S/C27H29N5O3/c1-2-23(33)31-16-13-18(14-17-31)22-12-15-29-27-24(26(28)34)25(30-32(22)27)19-8-10-21(11-9-19)35-20-6-4-3-5-7-20/h2-11,18,22,29H,1,12-17H2,(H2,28,34)/t22-/m0/s1 

 

Attribute
[Chem Name]	(7S)-2-(4-phenoxyphenyl)-7-(1-prop-2-enoylpiperidin-4-yl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide
[Synonym]	Zanubrutinib; BGB-3111
[CAS No.]	1691249-45-2
[MDL No.]	MFCD31567461
[Formula]	C27H29N5O3
[Molecular]	471.55
[Form]	Solid Powder
[Storage]	Sealed in dry. Store in freezer, under -20°C

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