Name | BGB-3111 |
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Synonyms |
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)-
7-(1-Acryloyl-4-piperidinyl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide |
Description | (±)-Zanubrutinib is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor. |
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Related Catalog | |
In Vitro | 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. (±)-Zanubrutinib is at least 10-fold weaker than ibrutinib in inhibiting rituximab induced ADCC, consistent with its weak ITK inhibition activity[1]. |
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[1]. |
References |
Density | 1.3±0.1 g/cm3 |
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Boiling Point | 713.4±60.0 °C at 760 mmHg |
Molecular Formula | C27H29N5O3 |
Molecular Weight | 471.551 |
Flash Point | 385.2±32.9 °C |
Exact Mass | 471.227051 |
LogP | 3.64 |
Vapour Pressure | 0.0±2.3 mmHg at 25°C |
Index of Refraction | 1.680 |