1354799-87-3
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- CAS号:
- 1354799-87-3
- 英文名:
- NS-018 (maleate)
- 英文别名:
- NS-018 (maleate);Ilginatinib maleate;NS018 MALEATE;ILGINATINIB MALEATE;ILGINATINIB (MALEATE) (NS-018 (MALEATE));(S)-N2-(1-(4-Fluorophenyl)ethyl)-4-(1-methyl-1H-pyrazol-4-yl)-N6-(pyrazin-2-yl)pyridine-2,6-diamine maleate;Inhibitor,JAK3,NS 018,inhibit,JAK2,Ilginatinib,bioavailable,NS018,orally,Ilginatinib maleate,NS-018,JAK1,Janus kinase,JAK,Tyk2
- 中文名:
- 1354799-87-3
- 中文别名:
- 化合物ILGINATINIB MALEATE;JAK2抑制剂(NS-018 MALEATE);(S)-N2-(1-(4-氟苯基)乙基)-4-(1-甲基-1H-吡唑-4-基)-N6-(吡嗪-2-基)吡啶-2,6-二胺 马来酸盐
- CBNumber:
- CB03137709
- 分子式:
- C25H24FN7O4
- 分子量:
- 505.5009632
- MOL File:
- 1354799-87-3.mol
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1354799-87-3化学性质
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储存条件:
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Store at -20°C
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溶解度:
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DMSO : ≥ 30 mg/mL (59.35 mM)
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形态:
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Solid
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颜色:
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Light yellow to yellow
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1354799-87-3性质、用途与生产工艺
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)。
JAK2
0.72 nM (IC
50
)
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Tyk2
22 nM (IC
50
)
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JAK1
33 nM (IC
50
)
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JAK3
39 nM (IC
50
)
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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.
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.
1354799-87-3
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
---|
2024/08/19 | HY-19631 | Ilginatinib maleate | | 1 mg | 900元 |
2024/08/19 | HY-19631 | 1354799-87-3 Ilginatinib maleate | 1354799-87-3 | 5mg | 2500元 |
1354799-87-3, 1354799-87-3 相关搜索:
- 抑制剂
- 细胞生物学试剂
- (S)-N2-(1-(4-氟苯基)乙基)-4-(1-甲基-1H-吡唑-4-基)-N6-(吡嗪-2-基)吡啶-2,6-二胺 马来酸盐
- 化合物ILGINATINIB MALEATE
- JAK2抑制剂(NS-018 MALEATE)
- 1354799-87-3
- (S)-N2-(1-(4-Fluorophenyl)ethyl)-4-(1-methyl-1H-pyrazol-4-yl)-N6-(pyrazin-2-yl)pyridine-2,6-diamine maleate
- Inhibitor,JAK3,NS 018,inhibit,JAK2,Ilginatinib,bioavailable,NS018,orally,Ilginatinib maleate,NS-018,JAK1,Janus kinase,JAK,Tyk2
- ILGINATINIB (MALEATE) (NS-018 (MALEATE))
- NS018 MALEATE;ILGINATINIB MALEATE
- Ilginatinib maleate
- NS-018 (maleate)