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Ilginatinib maleate

Name: Ilginatinib maleate
Brand: TargetMol
SKU: T12266L
Price: 41 USD
Availability: InStock
Rating: 5 (10 reviews)

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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

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Purity: 99.82%

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
1 mg	$41	In Stock
5 mg	$98	In Stock
10 mg	$137	In Stock
25 mg	$201	In Stock
50 mg	$289	In Stock
100 mg	$413	In Stock
200 mg	$548	In Stock
1 mL x 10 mM (in DMSO)	$109	In Stock

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Purity:99.82%

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COA HPLC

Product Introduction

Bioactivity

Description	Ilginatinib maleate (NS-018 maleate) is a highly active, orally bioavailable inhibitor of JAK2.
Targets&IC50	JAK2:0.72 nM, TYK2:22 nM, JAK3:39 nM, JAK1:33 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

Chemical Properties

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/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (98.91 mM), Sonication is recommended.

H2O: < 0.1 mg/mL (insoluble)

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.96 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9782 mL	9.8912 mL	19.7824 mL	98.9120 mL
5 mM	0.3956 mL	1.9782 mL	3.9565 mL	19.7824 mL
10 mM	0.1978 mL	0.9891 mL	1.9782 mL	9.8912 mL
20 mM	0.0989 mL	0.4946 mL	0.9891 mL	4.9456 mL
50 mM	0.0396 mL	0.1978 mL	0.3956 mL	1.9782 mL

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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 . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(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 TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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Tech Support

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