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Ilginatinib maleate

Catalog No. T12266L CAS 1354799-87-3

Synonyms: NS-018 maleate

Ilginatinib maleate (NS-018 maleate) is a highly active and orally bioavailable inhibitor of JAK2.

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Ilginatinib maleate, CAS 1354799-87-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 96.00
2 mg	In stock	$ 138.00
5 mg	In stock	$ 233.00
10 mg	In stock	$ 326.00
25 mg	In stock	$ 478.00
50 mg	In stock	$ 688.00
100 mg	In stock	$ 987.00
500 mg	In stock	$ 1,980.00
1 mL * 10 mM (in DMSO)	In stock	$ 259.00

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Purity: 99.68%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Ilginatinib maleate (NS-018 maleate) is a highly active and 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].

Synonyms	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: 30 mg/mL (59.35 mM)

H2O: < 0.1 mg/mL (insoluble)

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 Drug Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Tyrosine Kinase Inhibitor Library Bioactive Compounds Library Max Epigenetics Compound Library Anti-Cancer Compound Library Bioactive Compound Library Anti-Lung Cancer Compound Library

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Decernotinib SU 4981 Delgocitinib NVP-BSK805 2HCl (1092499-93-8(free base)) Zongertinib NVP-AEW541 RO495 BMS-911543

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Ilginatinib maleate 1354799-87-3 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors Tyrosine Kinases JAK Inhibitor JAK3 NS 018 inhibit JAK2 NS018 Maleate Ilginatinib NS-018 Maleate bioavailable NS018 orally NS-018 JAK1 Janus kinase NS-018 maleate Tyk2 NS 018 Maleate Ilginatinib Maleate inhibitor

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