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CCT241533 hydrochloride

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Catalog No. T10718LCas No. 1431697-96-9

CCT241533 hydrochloride is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM).

CCT241533 hydrochloride

CCT241533 hydrochloride

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Purity: 97.13%
Catalog No. T10718LCas No. 1431697-96-9
CCT241533 hydrochloride is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$67In StockIn Stock
2 mg$97In StockIn Stock
5 mg$162In StockIn Stock
10 mg$253In StockIn Stock
25 mg$542In StockIn Stock
50 mg$896In StockIn Stock
100 mg$1,330-In Stock
500 mg$2,680-In Stock
1 mL x 10 mM (in DMSO)$179In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:97.13%
Appearance:Solid
Color:White to Yellow
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Product Introduction

Bioactivity
Description
CCT241533 hydrochloride is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM).
Targets&IC50
Chk2:1.16 nM (Ki), Chk1:245 nM, Chk2:3 nM
In vitro
CCT241533 hydrochloride inhibits CHK2 (IC50: 3 nM) and shows minimal cross-reactivity against a panel of kinases at 1 μM. X-ray crystallography confirms that CCT241533 binds to CHK2 in the ATP pocket. CCT241533 blocks CHK2 activity in human tumor cell lines in response to DNA damage. CCT241533 does not potentiate the cytotoxicity of a selection of genotoxic agents in several cell lines. However, CCT241533 significantly potentiates the cytotoxicity of two structurally distinct PARP inhibitors. Clear induction of the pS516 CHK2 signal is seen with a PARP inhibitor alone and this activation is abolished by CCT241533. In HT-29, HeLa, and MCF-7, the cytotoxicity of CCT241533 (GI50) is 1.7, 2.2, and 5.1 μM, respectively [1]. CCT241533 hydrochloride is a potent CHK2 inhibitor (IC50: 3 nM), with selectivity (63-fold) over CHK1(IC50: 190 nM) and low hERG inhibition (IC50: 22 μM) [2].
Chemical Properties
Molecular Weight478.95
FormulaC23H28ClFN4O4
Cas No.1431697-96-9
SmilesCl.COc1cc2nc(nc(N[C@@H]3CNC[C@H]3C(C)(C)O)c2cc1OC)-c1cc(F)ccc1O
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 100 mg/mL (208.79 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.35 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
1mg5mg10mg50mg
1 mM2.0879 mL10.4395 mL20.8790 mL104.3950 mL
5 mM0.4176 mL2.0879 mL4.1758 mL20.8790 mL
10 mM0.2088 mL1.0440 mL2.0879 mL10.4395 mL
20 mM0.1044 mL0.5220 mL1.0440 mL5.2198 mL
50 mM0.0418 mL0.2088 mL0.4176 mL2.0879 mL
100 mM0.0209 mL0.1044 mL0.2088 mL1.0440 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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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

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