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CYT387 (momelotinib)硫酸盐

基本信息 产品图片 产品描述 供应商联系方式 同类产品

基本信息:

  • 发布时间: 2017-06-12
  • 产品名称: CYT387 (momelotinib)硫酸盐
  • 产品英文名称: CYT387 (momelotinib)
  • CAS号: 1056636-06-6
  • 产品包装: 10mg
  • 产品价格: 1252元/罐
  • 有效期: 一年

产品图片:

CYT387 (momelotinib)硫酸盐

产品描述:

CYT387 sulfate salt的生物活性

 

CYT387 sulfate(momelotinib) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3.
IC50 value: 11 nM/18 nM(JAK1/JAK2) [1]
Target: JAK1/JAK2
in vitro: CYT387 inhibits the proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated by IL-3 with IC50 of 1400 nM. Furthermore, CYT387 also causes the inhibition of cell proliferation in cell lines constitutively activated by JAK2 or MPL signaling, including Ba/F3-MPLW515L cells, CHRF-288-11 cells and Ba/F3-TEL-JAK2 cells with IC50 of 200 nM, 1 nM and 700 nM, respectively. In addition, CYT387 has been shown to inhibit erythroid colony growth in vitro from JAK2V617F-positive PV patients with similar potency with IC50 of 2μ-4 μM [1]. A recent study shows that CYT387 inhibits PI3K/AKT and Ras/MAPK signaling induced by IL-6 and IGF-1. Moreover, CYT387 induces apoptosis as a single agent and synergizes with the conventional anti-MM therapies bortezomib and melphalan in primary multiple myeloma (MM) cells [2].
in vivo: In a murine MPN model, CYT387 normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines [3].

 

化学信息

分子量
610.62
储存条件
参考CoA中推荐的条件进行储存。
分子式
C23H26N6O10S2
CAS号
1056636-06-6
溶剂/溶解度
DMSO

 

相关文献

 

[1]. Pardanani A, et al. CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients. Leukemia, 2009, 23(8), 1441-1445.

[2]. Monaghan KA, et al. The novel JAK inhibitor CYT387 suppresses multiple signalling pathways, prevents proliferation and induces apoptosis in phenotypically diverse myeloma cells. Leukemia, 2011, 25(12), 1891-1899.

[3]. Tyner JW, et al. CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood, 2010, 115(25), 5232-5240.

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  • 公司名称 深圳市浩博世纪生物有限公司
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