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Ilginatinib maleate
🥰Excellent
Catalog No. T12266LCas No. 1354799-87-3
Alias NS-018 maleate
Ilginatinib maleate (NS-018 maleate) is a highly active, orally bioavailable inhibitor of JAK2.
Ilginatinib maleate
🥰Excellent
Purity: 99.74%
Catalog No. T12266LAlias NS-018 maleateCas No. 1354799-87-3
Ilginatinib maleate (NS-018 maleate) is a highly active, orally bioavailable inhibitor of JAK2.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $58 | In Stock | |
| 5 mg | $140 | In Stock | |
| 10 mg | $196 | In Stock | |
| 25 mg | $287 | In Stock | |
| 50 mg | $413 | In Stock | |
| 100 mg | $592 | In Stock | |
| 200 mg | $783 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $155 | In Stock |
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Purity:99.74%
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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.Product Introduction
Bioactivity
Chemical Properties
| Description | Ilginatinib maleate (NS-018 maleate) is a highly active, orally bioavailable inhibitor of JAK2. |
| Targets&IC50 | JAK2:0.72 nM, JAK1:33 nM, TYK2:22 nM, JAK3:39 nM |
| 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 |
| Smiles | OC(=O)\C=C/C(O)=O.C[C@H](Nc1cc(cc(Nc2cnccn2)n1)-c1cnn(C)c1)c1ccc(F)cc1 |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (98.91 mM)  H2O: < 0.1 mg/mL (insoluble) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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