zanubrutinib NEW
Price | $57 | $147 | $263 |
Package | 1mg | 5mg | 10mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-19 |
Product Details
Product Name: zanubrutinib | CAS No.: 1691249-45-2 |
Purity: 99.74% | Supply Ability: 10g |
Release date: 2024/11/19 |
Product Introduction
Bioactivity
Name | zanubrutinib |
Description | Zanubrutinib (BGB-3111) is an inhibitor of Bruton tyrosine kinase (BTK). |
In vitro | In both biochemical and cellular assays, zanubrutinib demonstrated nanomolar BTK inhibition activity. In several MCL and DLBCL cell lines, zanubrutinib inhibited BCR aggregation-triggered BTK autophosphorylation, blocked downstream PLC-γ2 signaling, and potently inhibited cell proliferation. In comparison with ibrutinib, zanubrutinib 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, zanubrutinib 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 zanubrutinib resulted in a dose-dependent BTK occupancy and showed about 3-fold more potency than ibrutinib in target organs, including PBMC and spleen.zanubrutinib 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, zanubrutinib 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 zanubrutinib 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, zanubrutinib also demonstrated better anti-tumor activity than ibrutinib.Preliminary 14-day toxicity study in rats showed that zanubrutinib was very well tolerated and maximal tolerate dose (MTD) was not reached when it was dosed up to 250mg/kg/day[1]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 65 mg/mL (137.84 mM), Sonication is recommended. |
Keywords | Btk | zanubrutinib | BGB3111 | Inhibitor | BGB 3111 | inhibit | Bruton tyrosine kinase |
Inhibitors Related | evobrutinib | (±)-Zanubrutinib | CP-547632 | BMS-986142 | Edralbrutinib | Ibrutinib | IBT6A | Orelabrutinib | Atuzabrutinib | CGI-1746 |
Related Compound Libraries | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Kinase Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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