1633350-06-7
1633350-06-7 structure
- Name: (±)-Zanubrutinib
- Chemical Name: BGB-3111
- CAS Number: 1633350-06-7
- Molecular Formula: C27H29N5O3
- Molecular Weight: 471.551
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Btk
- Create Date: 2018-03-16 10:52:59
- Modify Date: 2025-08-26 18:41:10
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(±)-Zanubrutinib is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.
| Name | BGB-3111 |
|---|---|
| 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. |
|---|---|
| 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 |
|---|---|
| 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 |