1691249-45-2
1691249-45-2 structure
- Name: Zanubrutinib
- Chemical Name: Zanubrutinib
- CAS Number: 1691249-45-2
- Molecular Formula: C27H29N5O3
- Molecular Weight: 471.551
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Btk
- Create Date: 2018-04-21 07:56:33
- Modify Date: 2024-01-02 08:35:58
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Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor.
| Name | Zanubrutinib |
|---|---|
| Synonyms |
(7S)-7-(1-Acryloyl-4-piperidinyl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide
zanubrutinib 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)-, (7S)- AG9MHG098Z |
| Description | Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor. |
|---|---|
| Related Catalog | |
| Target |
BTK[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]. |
| 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]. |
| 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 |
| Storage condition | 2-8℃ |