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Ilginatinib hydrochloride

Catalog No. T12266L2 CAS 1239358-85-0

Synonyms: NS-018 hydrochloride

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

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Ilginatinib hydrochloride Chemical Structure

Ilginatinib hydrochloride, CAS 1239358-85-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 94.00
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	$ 219.00

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Purity: 99.55%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Ilginatinib hydrochloride (NS-018 hydrochloride) 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 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].

Synonyms	NS-018 hydrochloride
Molecular Weight	425.89
Formula	C21H21ClFN7
CAS No.	1239358-85-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 2 mg/mL (4.70 mM), Sonification is recommended.

DMSO: 35 mg/mL (82.18 mM)

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：

Tyrosine Kinase Inhibitor Library Inhibitor Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Clinical Compound Library Stem Cell Differentiation Compound Library Epigenetics Compound Library Anti-Liver Cancer Compound Library JAK-STAT Compound Library

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Related compounds with same targets

Cerdulatinib hydrochloride GTP-14564 Deucravacitinib Filgotinib Lorlatinib NVP-BSK805 2HCl (1092499-93-8(free base)) Larotinib Baricitinib

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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 hydrochloride 1239358-85-0 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors JAK Tyrosine Kinases Tyk2 Ilginatinib JAK1 NS 018 Hydrochloride JAK2 Inhibitor NS018 Hydrochloride bioavailable NS018 NS-018 Hydrochloride NS-018 orally inhibit Janus kinase JAK3 NS 018 Ilginatinib Hydrochloride NS-018 hydrochloride inhibitor

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