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Submit ReviewIbrutinib is a potent and selective BTK inhibitor (IC50= 0.5 nM). Selective for BTK against a screening panel of kinase enzymes. Inhibits autophosphorylation of BTK, phosphorylation of PLCγ, and phosphorylation of ERK (IC50 of 11 nM, 29 nM and 13 nM, respectively). Also inhibits ErbB4 (IC50 = 0.25-3.4 nM). Induces cytotoxicity of chronic lymphocytic leukemia (CLL) cells. Reduces clinical arthritis scores in a mouse model.
Ibrutinib is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Epigenetics Library and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
分子量 | 440.5 |
公式 | C25H24N6O2 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 936563-96-1 |
PubChem ID | 24821094 |
InChI Key | XYFPWWZEPKGCCK-GOSISDBHSA-N |
Smiles | NC1=C2C(N([C@@H]3CCCN(C(C=C)=O)C3)N=C2C4=CC=C(C=C4)OC5=CC=CC=C5)=NC=N1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 44.05 | 100 |
以下数据基于产品分子量 440.5。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.27 mL | 11.35 mL | 22.7 mL |
5 mM | 0.45 mL | 2.27 mL | 4.54 mL |
10 mM | 0.23 mL | 1.14 mL | 2.27 mL |
50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
参考文献是支持产品生物活性的出版物。
Honigberg et al (2010) The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc.Natl.Acad.Sci.USA 107 13075 PMID: 20615965
Pan et al (2007) Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase. Chem.Med.Chem. 2 58 PMID: 17154430
Estupiñán et al (2021) Comparative analysis of BTK inhibitors and mechanisms underlying adverse effects. Front.Cell Dev.Biol. 9 630942 PMID: 33777941
If you know of a relevant reference for Ibrutinib, please let us know.
关键词: Ibrutinib, Ibrutinib supplier, Potent, and, selective, Bruton, tyrosine, kinase, inhibitor, Btk, Brutons, Tyrosine, Kinase, (BTK), EGFR, 6813, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Ibrutinib 的部分引用包括:
John E et al (2021) Ibrutinib as a potential therapeutic for cocaine use disorder. Transl Psychiatry 11 623 PMID: 34880215
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