1354799-87-3
1354799-87-3 用途与合成方法
|
JAK2 0.72 nM (IC 50 ) |
Tyk2 22 nM (IC 50 ) |
JAK1 33 nM (IC 50 ) |
JAK3 39 nM (IC 50 ) |
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 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026-09-15 | HY-19631 | 1354799-87-3 | 1 mg | 490 | |
| 2026-09-15 | HY-19631 | 1354799-87-3 | 1354799-87-3 | 5mg | 997 |
