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NVP-BSK805

Name: NVP-BSK805
Brand: TargetMol
SKU: T5049
Rating: 4.5 (1 reviews)

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Catalog No. T5049Cas No. 1092499-93-8

NVP-BSK805 (BSK 805) is an ATP-competitive JAK2 inhibitor.

NVP-BSK805

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Catalog No. T5049Cas No. 1092499-93-8

NVP-BSK805 (BSK 805) is an ATP-competitive JAK2 inhibitor.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$57	7-10 days	7-10 days
5 mg	$133	7-10 days	7-10 days
10 mg	$220	7-10 days	7-10 days
25 mg	$432	7-10 days	7-10 days

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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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Appearance:Solid

Color:Yellow

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COA

Product Introduction

Bioactivity

Description	NVP-BSK805 (BSK 805) is an ATP-competitive JAK2 inhibitor.
Targets&IC50	FL JAK2 (V617F):0.56 nM, JAK1 JH1:31.63 nM, TYK2 JH1:10.76 nM, JAK3 JH1:18.68 nM, FL JAK2 (WT):0.58 nM, JAK2 JH1:0.48 nM
In vitro	GI50 of <100 nM. NVP-BSK805 blocks the STAT5 phosphorylation at ≥100 nM concentrations, and shows a bias for JAK2 over JAK1 and JAK3 inhibition in the JAK2V617F-mutant cell lines. NVP-BSK805 (5 μM) improves P-gp inhibitory activity. NVP-BSK805 increases sensitization of drug-resistant KBV20C cancer cells to VIC treatment at 10 μM, and such an effect is more effective than a 5 μM dose.
In vivo	NVP-BSK805 (150 mg/kg, p.o.) blocks STAT5 phosphorylation, splenomegaly, and leukemic cell spreading in a Ba/F3 JAK2V617F cell-driven mouse model. NVP-BSK805 (50, 75, and 100 mg/kg, p.o.) also suppresses rhEpo-mediated polycythemia and splenomegaly in BALB/c mice.

Chemical Properties

Molecular Weight	490.55
Formula	C₂₇H₂₈F₂N₆O
Cas No.	1092499-93-8
Smiles	Cl.Cl.Fc1cc(cc(F)c1CN1CCOCC1)-c1cccc2ncc(nc12)-c1cnn(c1)C1CCNCC1
Relative Density.	1.4 g/cm3

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: 10 mM, Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0385 mL	10.1926 mL	20.3853 mL	101.9264 mL
5 mM	0.4077 mL	2.0385 mL	4.0771 mL	20.3853 mL
10 mM	0.2039 mL	1.0193 mL	2.0385 mL	10.1926 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