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CHZ868

Name: CHZ868
Brand: TargetMol
SKU: TQ0061
Price: 67 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. TQ0061Cas No. 1895895-38-1

CHZ868 is a type II JAK inhibitor with potential antitumor activity that reverses the persistence of type I JAK inhibitors and can be used to study leukemia.

CHZ868

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Purity: 99.38%

Catalog No. TQ0061Cas No. 1895895-38-1

CHZ868 is a type II JAK inhibitor with potential antitumor activity that reverses the persistence of type I JAK inhibitors and can be used to study leukemia.

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
2 mg	$67	In Stock	In Stock
5 mg	Preferential	-	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:99.38%

Appearance:Solid

Color:White

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COA LCMS

Product Introduction

Bioactivity

Description	CHZ868 is a type II JAK inhibitor with potential antitumor activity that reverses the persistence of type I JAK inhibitors and can be used to study leukemia.
Targets&IC50	CMK cells:378 nM (GI50), JAK2:110 nM, SET2 cells:59 nM (GI50)
In vitro	CHZ868 effectively inhibits constitutive phosphorylation of JAK2 and STAT5 in JAK2V617F SET2 cells. The compound demonstrates potent inhibition of SET2 cell proliferation (GI50=59nM) and exhibits 6-fold lower growth inhibitory activity against CMK cells (GI50=378nM)[1]. At a concentration of 100 nM, CHZ868 shows activity against 26 kinases, including JAK2 and TYK2. It is believed that CHZ868 interacts with the hinge region of JAK2 through two hydrogen bonds, formed between the amino-pyridine of CHZ868 and the backbone-NH/CO of L932, while the pyridine occupies the adenine pocket of the ATP binding site. CHZ868 effectively suppresses the growth of CRLF2-rearranged human B-ALL cells and disrupts JAK2 signaling[1].
In vivo	Characterized by high passive permeability, good metabolic stability, and low water solubility, CHZ868 also exhibits moderate blood clearance and good oral bioavailability, rendering it suitable for in vivo applications. In mice with human or murine B-ALL, CHZ868 enhances survival. When used in combination with dexamethasone, CHZ868 synergistically induces apoptosis in JAK2-dependent B-ALLs, leading to improved survival compared to CHZ868 alone[1].
Cell Research	CHZ868 is dissolved in DMSO to make 10 mM stock solution and diluted in culture media. Cells are treated with CHZ868 (0, 0.05, 0.1, 0.2 μM) or vehicle (DMSO). After 48 hr (Ba/F3 cells) or 72 hr (MHH-CALL4 and PDX cells), CellTiter-Glo Luminescent Cell Viability Assay is added (10 μL undiluted or 25 μL of a 1:2 dilution in each well) and plates are read [2].
Animal Research	CHZ868 is reconstituted in 0.5% methylcellulose / 0.5% Tween-80 and administered at doses of 10 or 30 mg/kg/day by oral gavage. Pharmacokinetic/pharmacodynamic and efficacy studies in the mouse model of rhEpo-induced polycythemia are carried out essentially. Detection of STAT5 phosphorylation in spleen lysates by Meso Scale Discovery is performed [2].

Chemical Properties

Molecular Weight	423.42
Formula	C₂₂H₁₉F₂N₅O₂
Cas No.	1895895-38-1
Smiles	CC(=O)Nc1cc(Oc2ccc3n(C)c(Nc4ccc(F)cc4F)nc3c2C)ccn1
Relative Density.	1.37 g/cm3 (Predicted)

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: 50 mg/mL (118.09 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.72 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	2.3617 mL	11.8086 mL	23.6172 mL	118.0861 mL
5 mM	0.4723 mL	2.3617 mL	4.7234 mL	23.6172 mL
10 mM	0.2362 mL	1.1809 mL	2.3617 mL	11.8086 mL
20 mM	0.1181 mL	0.5904 mL	1.1809 mL	5.9043 mL
50 mM	0.0472 mL	0.2362 mL	0.4723 mL	2.3617 mL
100 mM	0.0236 mL	0.1181 mL	0.2362 mL	1.1809 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