| 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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : 2 mg/mL (4.70 mM), Sonication is recommended.
DMSO : 60 mg/mL (140.88 mM)
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| Keywords | Tyk2 | Ilginatinib | JAK1 | JAK | NS 018 Hydrochloride | JAK2 | Inhibitor | NS018 Hydrochloride | bioavailable | NS018 | NS-018 Hydrochloride | NS-018 | orally | inhibit | Janus kinase | JAK3 | Ilginatinib hydrochloride | NS 018 | Ilginatinib Hydrochloride |
| Inhibitors Related | Delgocitinib | Deucravacitinib | Fedratinib | Ruxolitinib | Tofacitinib Citrate | GSK 3 Inhibitor IX | Ibrutinib | Ruxolitinib phosphate | JAK-IN-10 | Baricitinib | Tofacitinib | Gefitinib |
| Related Compound Libraries | 经典已知活性库 | 酪氨酸激酶分子库 | 激酶抑制剂库 | 抗癌临床化合物库 | 药物功能重定位化合物库 | 抑制剂库 | 口服活性化合物库 | 临床期小分子药物库 | 已知活性化合物库 | 抗癌药物库 |
United States
