BGB-3111(Zanubrutinib)

Cas No.:	1691249-45-2
Chemical Name:	BGB-3111,Zanubrutinib
Synonyms:	BGB-3111,Zanubrutinib,BGB 3111,BGB3111
SMILES:	NC(C1=C2N(N=C1C3=CC=C(OC4=CC=CC=C4)C=C3)[C@H](C5CCN(C(C=C)=O)CC5)CCN2)=O
Formula:	C27H29N5O3
M.Wt:	471.55
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor.
In Vivo:	Zanubrutinib (BGB-3111) induces dose-dependent anti-tumor effects against REC-1 MCL xenografts engrafted either subcutaneously or systemically via tail vein injection in mice. In the subcutaneous xenografts, Zanubrutinib at 2.5 mg/kg BID shows similar activity as ibrutinib at 50 mg/kg QD. In the systemic model, the median survival of Zanubrutinib 25 mg/kg BID group is significantly longer than those of both ibrutinib 50 mg/kg QD and BID groups. In an ABC-subtype DLBCL (TMD-8) subcutaneous xenograft model, Zanubrutinib also demonstrates better anti-tumor activity than ibrutinib. Preliminary 14-day toxicity study in rats shows that Zanubrutinib is very well tolerated and maximal tolerate dose (MTD) is not reached when it is dosed up to 250 mg/kg/day[1].
In Vitro:	Zanubrutinib (BGB-3111) is a selective Bruton tyrosine kinase (BTK) inhibitor. In both biochemical and cellular assays, Zanubrutinib demonstrates nanomolar BTK inhibition activity. In several MCL and DLBCL cell lines, Zanubrutinib inhibits BCR aggregation-triggered BTK autophosphorylation, blocks downstream PLC-γ2 signaling, and potently inhibits cell proliferation. In comparison with ibrutinib, Zanubrutinib shows much more restricted off-target activities against a panel of kinases, including ITK[1].