| Name | Ilginatinib |
| Description | Ilginatinib (NS-018) is a highly active, orally bioavailable JAK2 inhibitor. |
| In vitro | Ilginatinib (NS-018) 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(NS-018) 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. |
| Solubility Information | DMSO : 50 mg/mL (128.39 mM), Sonication is recommended.
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| Keywords | JAK3 | Janus kinase | Inhibitor | JAK | NS018 | JAK2 | orally | Tyk2 | Ilginatinib | inhibit | NS 018 | JAK1 | bioavailable |
| Inhibitors Related | Delgocitinib | Deucravacitinib | Fedratinib | Ruxolitinib | Tofacitinib Citrate | GSK 3 Inhibitor IX | Ibrutinib | Ruxolitinib phosphate | JAK-IN-10 | Baricitinib | Tofacitinib | Gefitinib |
| Related Compound Libraries | Bioactive Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Stem Cell Differentiation Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
