(±)-Zanubrutinib

Research use only, not for human use.

The active enantiomer of Zanubrutinib (BGB3111), a potent, selective and orally available Btk inhibitor.

The active enantiomer of Zanubrutinib (BGB3111), a potent, selective and orally available Btk inhibitor; shows much more restricted off-target activities against a panel of kinases, including ITK, compared with Ibrutinib; demonstrates nanomolar BTK inhibition activity, inhibits BCR aggregation-triggered BTK autophosphorylation, blocks downstream PLC-γ2 signaling, and potently inhibits cell proliferation in several MCL and DLBCL cell lines; demonstrates better anti-tumor activity than ibrutinib in TMD-8 subcutaneous xenograft model.Blood Cancer Phase 3 Clinical.

In both biochemical and cellular assays, (±)-Zanubrutinib ((±)-BGB-3111) 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 PCI-32765, (±)-Zanubrutinib shows much more restricted off-target activities against a panel of kinases, including ITK.

(±)-Zanubrutinib 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. 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 250mg/kg/day.

±)-BGB-3111 | (±)-BGB 3111 | (±)-BGB3111

Tyrosine Kinase

BTK

BTK

Cancer

Blood cancer

1633350-06-7

471.55086

C27H29N5O3

>98% (HPLC)

10 mM in DMSO

NC(C1=C2N(N=C1C3=CC=C(OC4=CC=CC=C4)C=C3)C(C5CCN(C(C=C)=O)CC5)CCN2)=O

Pyrazolo[1,5-a]pyrimidine-3-carboxamide, 4,5,6,7-tetrahydro-7-[1-(1-oxo-2-propen-1-yl)-4-piperidinyl]-2-(4-phenoxyphenyl)-

(-20℃)

With Ice Pack

≥ 2 years