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Ilginatinib hydrochloride

Name: Ilginatinib hydrochloride
Brand: TargetMol
SKU: T12266L2
Price: 67 USD
Availability: InStock
Rating: 5 (10 reviews)

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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

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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 Size	Price	USA Warehouse	Global Warehouse
1 mg	$67	In Stock	In Stock
5 mg	$162	In Stock	In Stock
10 mg	$238	In Stock	In Stock
25 mg	$397	In Stock	In Stock
50 mg	$575	In Stock	In Stock
100 mg	$786	In Stock	In Stock
200 mg	$1,080	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$178	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.55%

Appearance:Viscous

Color:Yellow

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COA HNMR LCMS

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, JAK1:33 nM, JAK2:0.72 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

Chemical Properties

Molecular Weight	425.89
Formula	C₂₁H₂₁ClFN₇
Cas No.	1239358-85-0
Smiles	Cl.C[C@H](Nc1cc(cc(Nc2cnccn2)n1)-c1cnn(C)c1)c1ccc(F)cc1
Relative Density.	no data available

Storage & Solubility Information

Storage

Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 2 mg/mL (4.7 mM), Sonication is recommended.

DMSO: 60 mg/mL (140.88 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Saline: 2.5 mg/mL (5.87 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

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3480 mL	11.7401 mL	23.4802 mL	117.4012 mL

DMSO

	1mg	5mg	10mg	50mg
5 mM	0.4696 mL	2.3480 mL	4.6960 mL	23.4802 mL
10 mM	0.2348 mL	1.1740 mL	2.3480 mL	11.7401 mL
20 mM	0.1174 mL	0.5870 mL	1.1740 mL	5.8701 mL
50 mM	0.0470 mL	0.2348 mL	0.4696 mL	2.3480 mL
100 mM	0.0235 mL	0.1174 mL	0.2348 mL	1.1740 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 stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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

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