Description
(±)-Zanubrutinib ((±)-BGB-3111) is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.
Product information
CAS Number: 1633350-06-7
Molecular Weight: 471.55
Formula: C27H29N5O3
Chemical Name: 2-(4-phenoxyphenyl)-7-[1-(prop-2-enoyl)piperidin-4-yl]-4H,5H,6H,7H-pyrazolo[1,5-a]pyrimidine-3-carboxamide
Smiles: C=CC(=O)N1CCC(CC1)C1CCNC2=C(C(N)=O)C(=NN21)C1C=CC(=CC=1)OC1C=CC=CC=1
InChiKey: RNOAOAWBMHREKO-UHFFFAOYSA-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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 30 mg/mL (63.62 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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.
In Vivo:
(±)-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.
Products are for research use only. Not for human use.
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