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Zanubrutinib (BGB-3111) (Synonyms: BGB-3111)

Catalog No.GC34075

Zanubrutinib (BGB-3111) (BGB-3111) is a selective Bruton tyrosine kinase (Btk) inhibitor.

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Zanubrutinib (BGB-3111) Chemical Structure

Cas No.: 1691249-45-2

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10mM (in 1mL DMSO)
$149.00
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5mg
$162.00
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10mg
$288.00
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25mg
$576.00
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50mg
$923.00
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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

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Background

Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor.

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].

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].

[1]. Na Li, et al. Abstract 2597: BGB-3111 is a novel and highly selective Bruton's tyrosine kinase (BTK) inhibitor. Cancer Res 2015;75(15 Suppl):Abstract nr 2597.

Chemical Properties

Cas No. 1691249-45-2 SDF
Synonyms BGB-3111
Canonical SMILES NC(C1=C2N(N=C1C3=CC=C(OC4=CC=CC=C4)C=C3)[C@H](C5CCN(C(C=C)=O)CC5)CCN2)=O
Formula C27H29N5O3 M.Wt 471.55
Solubility DMSO : ≥ 56.75 mg/mL (120.35 mM);Ethanol : < 1 mg/mL (insoluble) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.1207 mL 10.6033 mL 21.2067 mL
5 mM 0.4241 mL 2.1207 mL 4.2413 mL
10 mM 0.2121 mL 1.0603 mL 2.1207 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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Reviews

Review for Zanubrutinib (BGB-3111)

Average Rating: 5 ★★★★★ (Based on Reviews and 5 reference(s) in Google Scholar.)

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