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Ilginatinib

Catalog No. T12266   CAS 1239358-86-1
Synonyms: NS-018

Ilginatinib is a highly active and orally bioavailable inhibitor of JAK2.

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Ilginatinib, CAS 1239358-86-1
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Purity: 98%
Biological Description
Chemical Properties
Storage & Solubility Information
Description Ilginatinib is a highly active and orally bioavailable inhibitor of JAK2.
Targets&IC50 JAK3:39 nM, Tyk2:22 nM, JAK1:33 nM, JAK2:0.72 nM
In vitro Ilginatinib (NS-018) 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(NS-018) 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].
Synonyms NS-018
Molecular Weight 389.43
Formula C21H20FN7
CAS No. 1239358-86-1

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 34 mg/mL (87.31 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Nakaya Y, et al. Efficacy of NS-018, a potent and selective JAK2/Src inhibitor, in primary cells and mouse models of myeloproliferative neoplasms. Blood Cancer J. 2011 Jul;1(7):e29. 2. Kuroda J, et al. NS-018, a selective JAK2 inhibitor, preferentially inhibits CFU-GM colony formation by bone marrow mononuclear cells from high-risk myelodysplastic syndrome patients. Leuk Res. 2014 May;38(5):619-24.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library Kinase Inhibitor Library Epigenetics Compound Library Angiogenesis related Compound Library JAK-STAT Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Bioactive Compound Library

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Ganoderic acid B Fedratinib hydrochloride hydrate Curculigoside FLLL32 Go6976 AZ960 Fosifidancitinib WDR5-0103

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