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  • DC Chemicals Limited
  • China
  • Product Name: BGB-3111
  • Price: $900.0/100mg $1800.0/250mg $3600.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

1633350-06-7

1633350-06-7 structure
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: 2024-01-14 10:21:58
  • (±)-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

[1]. Na L, et al. BGB-3111 is a novel and highly selective Bruton's tyrosine kinase (BTK) inhibitor. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 2597. doi:10.1158/1538-7445.AM2015-2597

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