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Gandotinib

Name: Gandotinib
Brand: TargetMol
SKU: T2638
Price: 47 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T2638Cas No. 1229236-86-5

Alias LY2784544

LY2784544(Gandotinib (LY2784544)) is a potent JAK2 inhibitor (IC50: 3 nM), effective in JAK2V617F(Ki: 0.245 nM). The selectivity is higher 8- and 20-fold than JAK1 and JAK3.

Gandotinib

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Purity: 99.86%

Catalog No. T2638Alias LY2784544Cas No. 1229236-86-5

LY2784544(Gandotinib (LY2784544)) is a potent JAK2 inhibitor (IC50: 3 nM), effective in JAK2V617F(Ki: 0.245 nM). The selectivity is higher 8- and 20-fold than JAK1 and JAK3.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$47	In Stock	In Stock
10 mg	$80	In Stock	In Stock
25 mg	$163	In Stock	In Stock
50 mg	$312	In Stock	In Stock
100 mg	$493	In Stock	In Stock
500 mg	$1,090	-	In Stock
1 mL x 10 mM (in DMSO)	$52	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:99.86%

Color:White

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COA HNMR HPLC

Product Introduction

Bioactivity

Description	LY2784544(Gandotinib (LY2784544)) is a potent JAK2 inhibitor (IC50: 3 nM), effective in JAK2V617F(Ki: 0.245 nM). The selectivity is higher 8- and 20-fold than JAK1 and JAK3.
Targets&IC50	Tyk2:44 nM, JAK3:48 nM, FGFR2:32 nM, FGFR3:106 nM, KDR:109 nM, ALK:138 nM, FLT3:4 nM, TRKB:95 nM, FLT4:25 nM, JAK2:3 nM, AURKA:168 nM, MAP3K9:299 nM, JAK2 (V617F):0.245 nM(Ki), MUSK:147 nM
In vitro	In severe combined immunodeficient mice, LY2784544 (administered orally) does not affect CD71/Ter119 positive erythroid progenitor cells within the spleen. LY2784544 significantly inhibits STAT5 phosphorylation in Ba/F3-JAK2 V617F-GFP xenografts (effective dose 50% [ED50]: 12.7 mg/kg). Additionally, in a JAK2 V617F-induced myeloproliferative neoplasm (MPN) model, LY2784544 (administered orally) reduces the tumor burden of Ba/F3-JAK2 V617F-GFP (ED50: 13.7 mg/kg).
In vivo	In proliferation assays, LY2784544 exhibits an anti-proliferative effect on JAK2 V617F-driven cells, with an IC50 of 68 nM. It demonstrates a less potent effect on cells driven by wild-type JAK2 and JAK3, with IC50 values of 1356 nM and 940 nM, respectively. LY2784544 also inhibits IL-3-activated wild-type JAK2 with an IC50 of 2.26 μM.
Cell Research	LY2784544 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. Ba/F3 cells expressing JAK2V617F are placed in RPMI-1640-containing vehicle (DMSO) or LY2784544 (concentration range, 0.001-20 μM) (1×104 cells/96-well). Ba/F3 cells expressing wild-type JAK2 are treated similarly except IL-3 (2 ng/mL) is added. After a 72-hour incubation, cell proliferation is assessed by adding Cell Titer 96 Aqueous One Solution Reagent (20 μL/well). The IC50 for inhibition of cell proliferation is calculated using the GraphPad Prism 4 software[1].
Synonyms	LY2784544

Chemical Properties

Molecular Weight	469.94
Formula	C₂₃H₂₅ClFN₇O
Cas No.	1229236-86-5
Smiles	C(C=1C=2N(C(CC3=C(F)C=C(Cl)C=C3)=C(C)N2)N=C(NC=4C=C(C)NN4)C1)N5CCOCC5
Relative Density.	1.45 g/cm3

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: 83.3 mg/mL (177.26 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 9 mg/mL (19.15 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.02 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

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1279 mL	10.6397 mL	21.2793 mL	106.3966 mL
5 mM	0.4256 mL	2.1279 mL	4.2559 mL	21.2793 mL
10 mM	0.2128 mL	1.0640 mL	2.1279 mL	10.6397 mL

DMSO

	1mg	5mg	10mg	50mg
20 mM	0.1064 mL	0.5320 mL	1.0640 mL	5.3198 mL
50 mM	0.0426 mL	0.2128 mL	0.4256 mL	2.1279 mL
100 mM	0.0213 mL	0.1064 mL	0.2128 mL	1.0640 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