Ilginatinib,1354799-87-3

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Ilginatinib maleate

CAS No. : 1354799-87-3

MCE 国际站：Ilginatinib maleate

产品活性：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)。

研究领域：Epigenetics  |  Protein Tyrosine Kinase/RTK  |  JAK/STAT Signaling  |  Stem Cell/Wnt

作用靶点：JAK

In Vitro: Ilginatinib maleate (NS-018 maleate) is a highly active JAK2 inhibitor, with an IC₅₀ of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC₅₀, 33 nM), JAK3 (IC₅₀, 39 nM), and Tyk2 (IC₅₀, 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 IC₅₀ 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.

In Vivo: 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.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Immunology/Inflammation Compound Library  |  JAK/STAT Compound Library  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Stem Cell Signaling Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Anti-COVID-19 Compound Library  |  Orally Active Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Anti-Obesity Compound Library  |  Anti-Liver Cancer Compound Library   |  Anti-Prostate Cancer Compound Library  |  Cancer Stem Cells Compound Library  |  Heterocyclic Compound Library  |  Pain-Related Compound Library  |  Autoimmune Disease Compound Library  |  Highly Selective Inhibitors Library  |  Ruxolitinib  |  Tofacitinib  |  Deucravacitinib  |  Baricitinib  |  AG490  |  Upadacitinib  |  Fedratinib  |  Pacritinib  |  Ritlecitinib  |  Momelotinib  |  WP1066  |  Filgotinib  |  Butyzamide  |  RO8191  |  AZD-1480  |  AT9283  |  Peficitinib  |  Abrocitinib  |  Itacitinib  |  Cucurbitacin I  |  CHZ868  |  (E/Z)-Zotiraciclib  |  Pyridone 6  |  Gandotinib  |  JAK2 JH2 Tracer  |  Atractylenolide I

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds