| Name | Ilginatinib maleate |
| Description | Ilginatinib maleate (NS-018 maleate) is a highly active, orally bioavailable inhibitor of JAK2. |
| In vitro | Ilginatinib maleate(NS-018 maleate) is highly active against JAK2 with a 50% inhibition (IC(50)) of <1 n, and had 30-50-fold greater selectivity for JAK2 over other JAK-family kinases, such as JAK1, JAK3 and tyrosine kinase 2.?In addition to JAK2, NS-018 inhibited Src-family kinases.?NS-018 showed potent antiproliferative activity against cell lines expressing a constitutively activated JAK2 (the JAK2V617F or MPLW515L mutations or the TEL-JAK2 fusion gene;?IC(50)=11-120 n), but showed only minimal cytotoxicity against most other hematopoietic cell lines without a constitutively activated JAK2[1]. |
| In vivo | Ilginatinib maleate(NS-018 maleate) preferentially suppressed in vitro erythropoietin-independent endogenous colony formation from polycythemia vera patients.?NS-018 also markedly reduced splenomegaly and prolonged the survival of mice inoculated with Ba/F3 cells harboring JAK2V617F.?In addition, NS-018 significantly reduced leukocytosis, hepatosplenomegaly and extramedullary hematopoiesis, improved nutritional status, and prolonged survival in JAK2V617F transgenic mice.?suggest that NS-018 will be a promising candidate for the treatment of MPNs[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 50 mg/mL (98.91 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.96 mM), Sonication is recommended.
H2O : < 0.1 mg/mL (insoluble)
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| Keywords | TyrosineKinases | Tyrosine Kinases | Tyk2 | orally | NS-018 Maleate | NS018 Maleate | NS-018 | NS018 | NS 018 Maleate | NS 018 | Janus kinase | JAK3 | JAK2 | JAK1 | JAK | Inhibitor | inhibit | Ilginatinib Maleate | Ilginatinib maleate | Ilginatinib | bioavailable |
| Inhibitors Related | Delgocitinib | Deucravacitinib | RO8191 | Tofacitinib Citrate | GSK 3 Inhibitor IX | CEP-33779 | Ibrutinib | Ruxolitinib phosphate | JAK-IN-10 | Fedratinib | Tofacitinib | Gefitinib |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Angiogenesis related Compound Library | Inhibitor Library | NO PAINS Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
