LFM-A13

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抑制剂描述：

产品名称：LFM-A13

产品别名：见爱必信官网

英文别名：LFM-A13

靶点：PLK

CAS：244240-24-2

纯度：>98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -80℃ for six months.

描述：FM-A13 is a selective inhibitor of Bruton’s tyrosine kinase (BTK) – IC??’s = 2.5 μM (recombinant BTK) and 17.2 μM (human BTK).

溶解性：DMSO 72 mg/mL warmed (200.0 mM)

体外研究：

In BTK+ B-lineage leukemic cells, LFM-A13 enhances their sensitivity to ceramide- or vincristine-induced apoptosis. In BCL-1 cells, NALM-6 cells, or normal BALB/c splenocytes, LFM-13 inhibits the enzymatic activity of BTK in BCL-1 cells without affecting the BTK protein expression levels In human neutrophils, LFM-A13 decreases the tyrosine phosphorylation induced by fMet-Leu-Phe and inhibits the production of superoxide anions and the stimulation of adhesion, chemotaxis, and phospholipase D activity.

体内研究：In BALB/c mice bearing BCL-1 leukemia, combination of LFM-A13 (50 mg/kg/day i.p.) and the standard triple-drug VPL prolongs the median survival time. In primary myeloma-bearing SCID-rab mice, LFM-A13 inhibits osteoclast activity, prevents myeloma-induced bone resorption and suppresss myeloma growth.

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