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CHR-6494

Name: CHR-6494
Brand: TargetMol
SKU: T14959
Price: 52 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T14959Cas No. 1333377-65-3

CHR-6494 is a haspin inhibitor that inhibits histone H3T3 phosphorylation (IC50: 2 nM).

CHR-6494

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Purity: 98.78%

Catalog No. T14959Cas No. 1333377-65-3

CHR-6494 is a haspin inhibitor that inhibits histone H3T3 phosphorylation (IC50: 2 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$52	In Stock	In Stock
10 mg	$79	In Stock	In Stock
25 mg	$156	In Stock	In Stock
50 mg	$288	In Stock	In Stock
100 mg	$490	In Stock	In Stock
200 mg	$715	-	In Stock
1 mL x 10 mM (in DMSO)	$58	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:98.78%

Color:Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	CHR-6494 is a haspin inhibitor that inhibits histone H3T3 phosphorylation (IC50: 2 nM).
Targets&IC50	Haspin:2 nM
In vitro	CHR-6494 does not modify H3S10 and H328 phosphorylation levels and shows no significantly inhibitory effects on other protein kinases. CHR-6494 dose-dependently inhibits the growth of cancer cells, such as HCT-116, HeLa, MDA-MB-231, and Wi-38 cell (IC50s: 500?nM, 473?nM, 752?nM, and 1059 nM). CHR-6494 (500 nM) produces a mitotic catastrophe with abnormal morphology of the mitotic spindle and centrosome amplification and upregulates the spindle assembly checkpoint protein BUB1 and the marker of mitotic arrest cyclin B1 [1]. CHR-6494 exhibits inhibitory activities against melanoma cell lines, including BRAFV600E mutants, NRAS mutants, and wild type cells, with IC50s ranging from 396 nM to 1229 nM. CHR-6494 (300 nM and 600 nM) induces apoptosis, increases caspase 3/7 activity by 3- and 6-fold, respectively in COLO-792 cells, and to 8.5- and 16-fold in RPMI-7951 cells. CHR-6494 in combination with MEK inhibitors synergistically inhibits the viability of melanoma cells, enhances apoptosis in melanoma cells, modulates cell cycle progression independently by arresting melanoma cells at different phases, and suppresses migration of melanoma cells [2].
In vivo	CHR-6494 (50?mg/kg, i.p.) inhibits the growth of tumor. It cuases no obvious body weight change in nude mice bearing HCT-116 human colorectal cancer cells [1].

Chemical Properties

Molecular Weight	292.34
Formula	C₁₆H₁₆N₆
Cas No.	1333377-65-3
Smiles	CCCNc(cc1)nn2c1ncc2c(cc3)cc4c3[nH]nc4
Relative Density.	1.39 g/cm3 (Predicted)

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: 50 mg/mL (171.03 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.84 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	3.4207 mL	17.1034 mL	34.2067 mL	171.0337 mL
5 mM	0.6841 mL	3.4207 mL	6.8413 mL	34.2067 mL
10 mM	0.3421 mL	1.7103 mL	3.4207 mL	17.1034 mL
20 mM	0.1710 mL	0.8552 mL	1.7103 mL	8.5517 mL
50 mM	0.0684 mL	0.3421 mL	0.6841 mL	3.4207 mL
100 mM	0.0342 mL	0.1710 mL	0.3421 mL	1.7103 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