1354799-87-3
- CAS号:1354799-87-3
- 英文名:NS-018 (maleate)
- 中文名:1354799-87-3
- CBNumber:CB03137709
- 分子式:C25H24FN7O4
- 分子量:505.5009632
- MOL File:1354799-87-3.mol
- 储存条件 :Store at -20°C
- 溶解度 :DMSO : ≥ 30 mg/mL (59.35 mM)
- 形态 :Solid
- 颜色 :Light yellow to yellow
1354799-87-3性质、用途与生产工艺
- 生物活性 Ilginatinib maleate (NS-018 maleate) 是一种高度有效的,可口服的 JAK2 抑制剂,IC50 值为 0.72 nM,对其选择性是对 JAK1 的 46 倍 (IC50, 33 nM),JAK3 的 54 倍 (IC50, 39 nM),以及 Tyk2 的 22 倍 (IC50, 22 nM)。
-
靶点
JAK2
0.72 nM (IC 50 )
Tyk2
22 nM (IC 50 )
JAK1
33 nM (IC 50 )
JAK3
39 nM (IC 50 )
-
体外研究
Ilginatinib maleate (NS-018 maleate) is a highly active JAK2 inhibitor, with an IC 50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC 50 , 33 nM), JAK3 (IC 50 , 39 nM), and Tyk2 (IC 50 , 22 nM). Ilginatinib maleate also inhibits Src-family kinases, especially SRC and FYN, and weakly inhibits ABL and FLT3 with 45- and 90-fold selectivity for JAK2, respectively. Ilginatinib maleate shows potent inhibitory activity against cell lines JAK2V617F or MPLW515L mutations or the TEL-JAK2 fusion gene (expressing a constitutively activated JAK2) with IC 50 of 11-120 nM, but has only minimal cytotoxicity against most other hematopoietic cell lines that have no constitutively activated JAK2.
Ilginatinib maleate (0.5 μM) preferentially suppresses colony-forming unitgranulocyte/macrophage (CFU-GM) formation from myelodysplastic syndrome (MDS)-derived bone marrow mononuclear cells (BMMNCs). Ilginatinib maleate (1 μM) suppresses the phosphorylation of STAT3 (the downstream kinase of JAK2) in CFU-GM-forming cells from MDS patients. -
体内研究
Ilginatinib maleate (NS-018 maleate) (12.5, 25, 50, 100 mg/kg, p.o.) potently prolongs the survival of mice and reduces splenomegaly in a mouse Ba/F3-JAK2V617F disease model.
Ilginatinib maleate (25, 50 mg/kg, p.o.) significantly reduces leukocytosis, hepatosplenomegaly and extramedullary hematopoiesis, improves nutritional status, and prolongs survival in JAK2V617F transgenic mice.
- 更新日期:2024/04/30
- 产品编号:HY-19631
- 产品名称:Ilginatinib maleate
- CAS编号:
- 包装:1 mg
- 价格:900元
- 更新日期:2024/04/30
- 产品编号:HY-19631
- 产品名称:1354799-87-3 Ilginatinib maleate
- CAS编号:1354799-87-3
- 包装:10mM * 1mLin DMSO
- 价格:2780元
- 公司名称:MedChemexpress LLC
- 联系电话:021-58955995
- 电子邮件:sales@medchemexpress.cn
- 国家:美国
- 产品数:4863
- 优势度:58
- 公司名称:Musechem
- 联系电话:+1-800-259-7612
- 电子邮件:info@musechem.com
- 国家:美国
- 产品数:4662
- 优势度:60
- 公司名称:TargetMol Chemicals Inc.
- 联系电话:+1-781-999-5354 +1-00000000000
- 电子邮件:marketing@targetmol.com
- 国家:美国
- 产品数:19892
- 优势度:58
- 公司名称:MedChemExpress
- 联系电话:--
- 电子邮件:sales@medchemexpress.com
- 国家:美国
- 产品数:6398
- 优势度:58