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Submit ReviewLFM-A13 is a potent and selective inhibitor of Bruton's tyrosine kinase (BTK). Inhibits recombinant BTK with an IC50 value of 2.5 μM and has no activity on other protein kinases ( including JAK1, JAK3, HCK, EGFR kinase and insulin receptor kinase) at concentrations of up to 278 μM.
LFM-A13 is also offered as part of the Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
分子量 | 360 |
公式 | C11H8Br2N2O2 |
储存 | Store at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 62004-35-7 |
PubChem ID | 54676905 |
InChI Key | UVSVTDVJQAJIFG-VURMDHGXSA-N |
Smiles | C\C(O)=C(/C#N)C(=O)NC1=C(Br)C=CC(Br)=C1 |
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 | 36 | 100 |
以下数据基于产品分子量 360。 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 | 2.78 mL | 13.89 mL | 27.78 mL |
5 mM | 0.56 mL | 2.78 mL | 5.56 mL |
10 mM | 0.28 mL | 1.39 mL | 2.78 mL |
50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
参考文献是支持产品生物活性的出版物。
Crosby and Pool (2002) Interaction of Bruton's tyrosine kinase and protein kinase Cθ in platelets. J.Biol.Chem. 277 9958 PMID: 11788586
Mahajan et al (1999) Rational design and synthesis of a novel anti-leukemic agent targeting Bruton's tyrosine kinase (BTK), LFM-A13 [α-cyano-β-hydroxy-β-methyl-N-(2,5-dibromophenyl)propenamide]. J.Biol.Chem. 274 9587 PMID: 10092645
Vassilev et al (1999) Bruton's tyrosine kinase as an inhibitor of the Fas/CD95 death-inducing signaling complex. J.Biol.Chem. 274 1646 PMID: 9880544
If you know of a relevant reference for LFM-A13, please let us know.
关键词: LFM-A13, LFM-A13 supplier, Potent, selective, BTK, inhibitors, inhibits, Brutons, Tyrosine, Kinases, LFMA13, Kinase, (BTK), 1300, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 LFM-A13 的部分引用包括:
He et al (2016) NEK7 is an essential mediator of NLRP3 activation downstream of potassium efflux. Nature 530 354 PMID: 26814970
Tankiewicz-Kwedlo et al (2018) Erythropoietin Intensifies the Proapoptotic Activity of LFM-A13 in Cells and in a Mouse Model of Colorectal Cancer. Int J Mol Sci 19 PMID: 29690619
Colmers and Bains (2018) Balancing tonic and phasic inhibition in hypothalamic CRH-releasing hormone neurons. J Physiol 596 1919 PMID: 29419884
Hart et al (2011) Essential role of Stat3 in PI3K-induced oncogenic transformation. Pain 108 13247 PMID: 21788516
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