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1354799-87-3

中文名稱 1354799-87-3
英文名稱 NS-018 (maleate)
CAS 1354799-87-3
分子式 C25H24FN7O4
分子量 505.501
MOL 文件 1354799-87-3.mol
更新日期 2024/11/15 18:20:30
1354799-87-3 結(jié)構(gòu)式 1354799-87-3 結(jié)構(gòu)式

基本信息

中文別名
化合物ILGINATINIB MALEATE
JAK2抑制劑(NS-018 MALEATE)
英文別名
NS-018 (maleate)
Ilginatinib maleate
NS018 MALEATE
ILGINATINIB MALEATE
ILGINATINIB (MALEATE) (NS-018 (MALEATE))

物理化學(xué)性質(zhì)

儲存條件-20°C儲存
溶解度DMSO : ≥ 30 mg/mL (59.35 mM)
形態(tài)Solid
顏色Light yellow to yellow
1354799-87-3價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2025/12/22HY-19631Ilginatinib maleate1354799-87-31 mg490元
2025/12/22HY-196311354799-87-3
Ilginatinib maleate
1354799-87-35mg997元
2025/12/22HY-196311354799-87-3
Ilginatinib maleate
1354799-87-310mM * 1mLin DMSO1109元

常見問題列表

生物活性
Ilginatinib maleate (NS-018 maleate) 是一種高度有效的,可口服的 JAK2 抑制劑,IC50 值為 0.72 nM,對其選擇性是對 JAK1 的 46 倍 (IC50, 33 nM),JAK3 的 54 倍 (IC50, 39 nM),以及 Tyk2 的 22 倍 (IC50, 22 nM)。
靶點

JAK2

0.72 nM (IC 50 )

Tyk2

22 nM (IC 50 )

JAK1

33 nM (IC 50 )

JAK3

39 nM (IC 50 )

體外研究

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.

體內(nèi)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.

"1354799-87-3" 相關(guān)產(chǎn)品信息
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