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Ilginatinib maleate
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Ilginatinib maleate
Catalog No. T12266LCas No. 1354799-87-3
Ilginatinib maleate (NS-018 maleate) is a highly active and orally bioavailable inhibitor of JAK2.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $96 | In Stock | |
| 2 mg | $138 | In Stock | |
| 5 mg | $233 | In Stock | |
| 10 mg | $326 | In Stock | |
| 25 mg | $478 | In Stock | |
| 50 mg | $688 | In Stock | |
| 100 mg | $987 | In Stock | |
| 500 mg | $1,980 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $259 | In Stock |
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Ilginatinib maleate (NS-018 maleate) is a highly active and 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]. |
| Alias | NS-018 maleate |
| Molecular Weight | 505.5 |
| Formula | C25H24FN7O4 |
| Cas No. | 1354799-87-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | ||||||||||
| Solubility Information | DMSO: 50 mg/mL (98.91 mM)  H2O: < 0.1 mg/mL (insoluble) | ||||||||||
Solution Preparation Table | |||||||||||
DMSO
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