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zanubrutinib

Catalog No. T7584 CAS 1691249-45-2

Synonyms: BGB-3111

Zanubrutinib (BGB-3111) is an inhibitor of Bruton tyrosine kinase (BTK).

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zanubrutinib, CAS 1691249-45-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 57.00
2 mg	In stock	$ 83.00
5 mg	In stock	$ 147.00
10 mg	In stock	$ 263.00
25 mg	In stock	$ 597.00
50 mg	In stock	$ 852.00
100 mg	In stock	$ 1,170.00
500 mg	In stock	$ 2,350.00
1 mL * 10 mM (in DMSO)	In stock	$ 153.00

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Purity: 99.74%

Purity: 99.24%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Zanubrutinib (BGB-3111) is an inhibitor of Bruton tyrosine kinase (BTK).
In vitro	In both biochemical and cellular assays, BGB-3111 demonstrated nanomolar BTK inhibition activity. In several MCL and DLBCL cell lines, BGB-3111 inhibited BCR aggregation-triggered BTK autophosphorylation, blocked downstream PLC-γ2 signaling, and potently inhibited cell proliferation. In comparison with ibrutinib, BGB-3111 showed much more restricted off-target activities against a panel of kinases, including ITK. While ibrutinib significantly inhibited rituximab-induced NK cell IFN-γ secretion and in vitro cytotoxicity on mantle cell lymphoma cells, BGB-3111 was at least 10-fold weaker than ibrutinib in inhibiting rituximab induced ADCC, consistent with its weak ITK inhibition activity[1].
In vivo	In mouse BTK occupancy assays, treatment with BGB-3111 resulted in a dose-dependent BTK occupancy and showed about 3-fold more potency than ibrutinib in target organs, including PBMC and spleen.?BGB-3111 induced 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, BGB-3111 at 2.5 mg/kg BID showed similar activity as ibrutinib at 50 mg/kg QD, its clinical relevant dose.?In the systemic model, the median survival of BGB-3111 25 mg/kg BID group was significantly longer than those of both ibrutinib 50 mg/kg QD and BID groups.?In an ABC-subtype DLBCL (TMD-8) subcutaneous xenograft model, BGB-3111 also demonstrated better anti-tumor activity than ibrutinib.?Preliminary 14-day toxicity study in rats showed that BGB-3111 was very well tolerated and maximal tolerate dose (MTD) was not reached when it was dosed up to 250mg/kg/day[1].

Synonyms	BGB-3111
Molecular Weight	471.55
Formula	C27H29N5O3
CAS No.	1691249-45-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 56.75 mg/mL (120.35 mM)

References and Literature

1. Li N , Sun Z , Liu Y , et al. Abstract 2597: BGB-3111 is a novel and highly selective Bruton's tyrosine kinase (BTK) inhibitor[J]. Cancer Research, 2015, 75(15 Supplement):2597-2597. 2. Chiara Tarantelli, Lu Zhang, Elisabetta Curti ,et al.The Bruton Tyrosine Kinase Inhibitor Zanubrutinib (BGB-3111) Demonstrated Synergies With Other Anti-Lymphoma Targeted Agents[J].Haematologica, 104 (7), e307-e309 Jul 2019

Related compound libraries

This product is contained In the following compound libraries：

EMA Approved Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Highly Selective Inhibitor Library Tyrosine Kinase Inhibitor Library Inhibitor Library Cysteine Covalent Library

Related Products

Related compounds with same targets

ONO-4059 analog GDC-0834 XMU-MP-2 Btk inhibitor 2 (±)-Zanubrutinib RSH-7 Rilzabrutinib CGI-1746

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

zanubrutinib 1691249-45-2 Angiogenesis Tyrosine Kinase/Adaptors BTK Btk BGB3111 BGB-3111 Inhibitor BGB 3111 inhibit Bruton tyrosine kinase inhibitor

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