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BMS-911543
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMS-911543图片
CAS NO:1271022-90-2
规格:98%
分子量:432.52
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
JAK2 inhibitor,selective small molecule
CAS:1271022-90-2
分子式:C23H28N8O
分子量:432.52
纯度:98%
存储:Store at -20°C

Background:

BMS-911543 is a selective small-molecule inhibitor of JAK2 with IC50 value of 1.1nM [1].


BMS-911543 is a reversible pyrrolopyridine ATP-competitive JAK2 inhibitor with a high selectivity. In the in vitro assay using human recombinant JAK enzyme, BMS-911543 displays an IC50 value of 1.1nM against JAK2 and the Ki value is 0.48nM. The inhibition activity and affinity against JAK2 are both much higher than those against JAK1 and JAK3. Besides that, BMS-911543 also has efficacy against other kinases, such as Lyn and the c-FMS receptor tyrosine kinase. In JAK-dependent cells such as SET2 or Ba/F3, the treatment of BMS-911543 causes an anti-proliferative effect with IC50 values of 60 and 70nM, respectively. The cell lines depending on other JAK family members do not show significant anti-proliferative response to BMS-911543. The colony growth assays prove that BMS-911543 can suppress the growth of MPN patient-derived cells and is more potent in the JAK2V617F pathway compared with the JAK2WT pathway. BMS-911543 is also found to be potent in vivo in both the JAK2WT pathway and the JAK2V617F pathway through suppressing pSTAT5 induction [1].


参考文献:
[1] Purandare AV, McDevitt TM, Wan H, You D, Penhallow B, Han X, Vuppugalla R, Zhang Y, Ruepp SU, Trainor GL, Lombardo L, Pedicord D, Gottardis MM, Ross-Macdonald P, de Silva H, Hosbach J, Emanuel SL, Blat Y, Fitzpatrick E, Taylor TL, McIntyre KW, Michaud E, Mulligan C, Lee FY, Woolfson A, Lasho TL, Pardanani A, Tefferi A, Lorenzi MV. Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2. Leukemia. 2012 Feb;26(2):280-8.