| Name | Ilginatinib hydrochloride |
| Description | Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active, orally bioavailable JAK2 inhibitor. |
| In vitro | Ilginatinib hydrochloride(NS-018 hydrochloride) 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 hydrochloride(NS-018 hydrochloride) 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 | Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : 2 mg/mL (4.7 mM), Sonication is recommended.
DMSO : 60 mg/mL (140.88 mM), Sonication is recommended.
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| Keywords | TyrosineKinases | Tyrosine Kinases | Tyk2 | orally | NS-018 Hydrochloride | NS018 Hydrochloride | NS-018 | NS018 | NS 018 Hydrochloride | NS 018 | Janus kinase | JAK3 | JAK2 | JAK1 | JAK | Inhibitor | inhibit | Ilginatinib hydrochloride | Ilginatinib Hydrochloride | Ilginatinib | bioavailable |
| Inhibitors Related | Deucravacitinib | RO8191 | Ruxolitinib | Tofacitinib Citrate | GSK 3 Inhibitor IX | CEP-33779 | Ibrutinib | Ruxolitinib phosphate | JAK-IN-10 | Fedratinib | Gefitinib | Upadacitinib |
| Related Compound Libraries | Apoptosis Compound Library | Reprogramming Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
