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Ilginatinib hydrochloride

Catalog No. T12266L2Cas No. 1239358-85-0
Alias NS-018 hydrochloride

Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active, orally bioavailable JAK2 inhibitor.

Ilginatinib hydrochloride

Ilginatinib hydrochloride

Purity: 99.55%
Catalog No. T12266L2Alias NS-018 hydrochlorideCas No. 1239358-85-0
Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active, orally bioavailable JAK2 inhibitor.
Pack SizePriceAvailabilityQuantity
1 mg$94In Stock
5 mg$233In Stock
10 mg$326In Stock
25 mg$478In Stock
50 mg$688In Stock
100 mg$987In Stock
500 mg$1,980In Stock
1 mL x 10 mM (in DMSO)$219In Stock
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Purity:99.55%
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Product Introduction

Bioactivity
Description
Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active, orally bioavailable JAK2 inhibitor.
Targets&IC50
JAK3:39 nM, TYK2:22 nM, JAK2:0.72 nM, JAK1:33 nM
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].
AliasNS-018 hydrochloride
Chemical Properties
Molecular Weight425.89
FormulaC21H21ClFN7
Cas No.1239358-85-0
Storage & Solubility Information
StoragePowder: -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)
Solution Preparation Table
H2O/DMSO
1mg5mg10mg50mg
1 mM2.3480 mL11.7401 mL23.4802 mL117.4012 mL
DMSO
1mg5mg10mg50mg
5 mM0.4696 mL2.3480 mL4.6960 mL23.4802 mL
10 mM0.2348 mL1.1740 mL2.3480 mL11.7401 mL
20 mM0.1174 mL0.5870 mL1.1740 mL5.8701 mL
50 mM0.0470 mL0.2348 mL0.4696 mL2.3480 mL
100 mM0.0235 mL0.1174 mL0.2348 mL1.1740 mL

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