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CHR-6494 TFA

Name: CHR-6494 TFA
Brand: TargetMol
SKU: T9521
Price: 58 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T9521Cas No. 1458630-17-5

CHR-6494 TFA is a potent haspin inhibitor with an IC50 of 2 nM, inhibiting histone H3T3 phosphorylation. It induces apoptosis in cancer cells, including melanoma and breast cancer, and is useful for cancer research.

CHR-6494 TFA

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Purity: 99.50%

Catalog No. T9521Cas No. 1458630-17-5

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$58	In Stock	In Stock
5 mg	$130	In Stock	In Stock
10 mg	$211	In Stock	In Stock
25 mg	$353	In Stock	In Stock
50 mg	$503	In Stock	In Stock
100 mg	$696	In Stock	In Stock
200 mg	$938	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$153	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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Batch Information

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Purity:99.50%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	CHR-6494 TFA is a potent haspin inhibitor with an IC50 of 2 nM, inhibiting histone H3T3 phosphorylation. It induces apoptosis in cancer cells, including melanoma and breast cancer, and is useful for cancer research.
Targets&IC50	Haspin:2 nM (IC50)
In vitro	Administration of CHR-6494 (TFA; 0-10-5?nM; 72 hours) dose-dependently inhibits the growth of cancer cells, such as HCT-116, HeLa, MDA-MB-231, and Wi-38 cells, with an IC50s of 500?nM, 473?nM, 752?nM and 1059 nM, respectively[1]. Administration of CHR-6494 (TFA; 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].
In vivo	Administration of CHR-6494 (TFA; 50?mg/kg; i.p. in two cycles of five consecutive days for 15 days) inhibits the growth of tumor and no obvious body weight change is observed in nude mice bearing HCT-116 human colorectal cancer cells[1].

Chemical Properties

Molecular Weight	406.36
Formula	C₁₈H₁₇F₃N₆O₂
Cas No.	1458630-17-5
Smiles	CCCNC1=NN2C(C=C1)=NC=C2C3=CC4=C(NN=C4)C=C3.O=C(O)C(F)(F)F
Relative Density.	1.31g/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: 55 mg/mL (135.35 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4609 mL	12.3044 mL	24.6087 mL	123.0436 mL
5 mM	0.4922 mL	2.4609 mL	4.9217 mL	24.6087 mL
10 mM	0.2461 mL	1.2304 mL	2.4609 mL	12.3044 mL
20 mM	0.1230 mL	0.6152 mL	1.2304 mL	6.1522 mL
50 mM	0.0492 mL	0.2461 mL	0.4922 mL	2.4609 mL
100 mM	0.0246 mL	0.1230 mL	0.2461 mL	1.2304 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