LFM-A13
發(fā)布者：信康 瀏覽次數(shù)：
產(chǎn)品名稱:LFM-A13CAS:244240-24-2別名：(2Z)-2-氰基-N-(2,5-二溴苯基)-3-羥基-2-丁烯酰胺英文名：LFM-A13
- 儲存條件 −20°C
- 溶解度 DMSO: 15 mg/mL
- 形態(tài)powder
- 顏色white
- 生物活性LFM-A13是一種特異性布魯頓氏酪氨酸激酶(BTK)，IC50為2.5 μM,選擇性比其他蛋白激酶，包括JAK1，JAK2，HCK，EGFR，和 IRK高100多倍。
- 體外研究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.
- 體內(nèi)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.
