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Ensartinib

Name: Ensartinib
Brand: TargetMol
SKU: T37585
Price: 52 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T37585Cas No. 1370651-20-9

Alias X-396, X396, Ensacove

Ensartinib (X-396) is a potent and orally active dual ALK/MET inhibitor for the treatment of ALK-positive non-small cell lung cancer (NSCLC).

Ensartinib

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Purity: 99.92%

Catalog No. T37585Alias X-396, X396, EnsacoveCas No. 1370651-20-9

Ensartinib (X-396) is a potent and orally active dual ALK/MET inhibitor for the treatment of ALK-positive non-small cell lung cancer (NSCLC).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$52	-	In Stock
5 mg	$123	-	In Stock
10 mg	$197	-	In Stock
25 mg	$396	-	In Stock
50 mg	$645	-	In Stock
100 mg	$987	-	In Stock
200 mg	$1,390	-	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:99.92%

Appearance:Solid

Color:White

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	Ensartinib (X-396) is a potent and orally active dual ALK/MET inhibitor for the treatment of ALK-positive non-small cell lung cancer (NSCLC).
Targets&IC50	ALK:13.4 nM
In vitro	Ensartinib is a potent ALK inhibitor that exhibits strong antiproliferative activity in various EML4-ALK–positive NSCLC cell lines. In H3122 cells, Ensartinib (IC₅₀ = 13.4 nM) significantly suppressed proliferation and induced PARP cleavage and apoptosis. Ensartinib also blocked ALK autophosphorylation and downstream signaling via AKT and ERK, indicating robust ALK pathway inhibition[1].
In vivo	In H3122 xenograft mouse models, oral administration of Ensartinib (50 or 100 mg/kg, once daily for 14 days) significantly inhibited tumor growth (p < 0.001), with complete tumor regression observed in some mice at the 100 mg/kg dose. Ensartinib demonstrated good oral bioavailability, potent ALK targeting in vivo, and low toxicity.[1].
Cell Research	For viability experiments, cells are seeded in 96-well plates at 25%-33% confluency and exposed to drugs.The human lung adenocarcinoma cell lines H3122 and H2228 are treated with Ensartinib (10, 30, 100, 300 and 1000 nM). SUDHL-1 lymphoma cells are treated with Ensartinib (5, 10, 30, 100 and 300 nM). SY5Y neuroblastoma cells are treated with Ensartinib (30, 100, 300 and 1000 nM). At 72 hours post Ensartinib addition, Cell Titer Blue Reagent is added and fluorescence is measured on a Spectramax spectrophotometer. All experimental points are set up in hextuplicate replicates and are performed at least two independent times. IC50s are calculated using GraphPad Prism version 5 for Windows. The curves are fit using a nonlinear regression model with a log (inhibitor) vs. response formula[1].
Synonyms	X-396, X396, Ensacove

Chemical Properties

Molecular Weight	561.44
Formula	C₂₆H₂₇Cl₂FN₆O₃
Cas No.	1370651-20-9
Smiles	C(=O)(N1C[C@@H](C)N[C@@H](C)C1)C2=CC=C(NC(=O)C3=CC(O[C@H](C)C4=C(Cl)C(F)=CC=C4Cl)=C(N)N=N3)C=C2
Relative Density.	no data available

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 80 mg/mL (142.49 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (5.88 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	1.7811 mL	8.9057 mL	17.8113 mL	89.0567 mL
5 mM	0.3562 mL	1.7811 mL	3.5623 mL	17.8113 mL
10 mM	0.1781 mL	0.8906 mL	1.7811 mL	8.9057 mL
20 mM	0.0891 mL	0.4453 mL	0.8906 mL	4.4528 mL
50 mM	0.0356 mL	0.1781 mL	0.3562 mL	1.7811 mL
100 mM	0.0178 mL	0.0891 mL	0.1781 mL	0.8906 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