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GDC-0425

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Catalog No. T9666Cas No. 1200129-48-1
Alias RG-7602

GDC-0425 (RG-7602) is a potent and highly selective inhibitor of Checkpoint kinase 1 (Chk1). This product blocks DNA damage-induced cell cycle arrest by inhibiting Chk1 activity, forcing damaged cells into mitosis and ultimately leading to apoptosis. Research indicates that the activity of GDC-0425 is modulated by the Ras-MEK signaling pathway, and it significantly enhances tumor regression when combined with DNA-damaging agents like Gemcitabine.

GDC-0425

GDC-0425

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Catalog No. T9666Alias RG-7602Cas No. 1200129-48-1
GDC-0425 (RG-7602) is a potent and highly selective inhibitor of Checkpoint kinase 1 (Chk1). This product blocks DNA damage-induced cell cycle arrest by inhibiting Chk1 activity, forcing damaged cells into mitosis and ultimately leading to apoptosis. Research indicates that the activity of GDC-0425 is modulated by the Ras-MEK signaling pathway, and it significantly enhances tumor regression when combined with DNA-damaging agents like Gemcitabine.
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2 mg$149-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
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:White
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Product Introduction

Bioactivity
Description
GDC-0425 (RG-7602) is a potent and highly selective inhibitor of Checkpoint kinase 1 (Chk1). This product blocks DNA damage-induced cell cycle arrest by inhibiting Chk1 activity, forcing damaged cells into mitosis and ultimately leading to apoptosis. Research indicates that the activity of GDC-0425 is modulated by the Ras-MEK signaling pathway, and it significantly enhances tumor regression when combined with DNA-damaging agents like Gemcitabine.
In vitro
GDC-0425 dose-dependently inhibits proliferation (0.001-10 mM, 72 h) and induces Chk1 hyperphosphorylation (3 µM, 24 h) in Chk1-positive breast cancer cells. Mechanistic studies demonstrate that GDC-0425-mediated cell death is dependent on Ras-MEK signaling, as blocking this pathway via MEK inhibition or RNAi protects cells from viability loss [3].
In vivo
In NCr nude mice bearing osteosarcoma (143B) or TNBC (HCC1806, HCC70) xenografts, oral GDC-0425 (50-75 mg/kg) partially inhibits tumor growth. Combined treatment with GDC-0425 (administered at 24, 48, and 72 h post-chemo) and Gemcitabine (120 mg/kg, i.p.) leads to significant tumor regression across all models [3].
SynonymsRG-7602
Chemical Properties
Molecular Weight321.38
FormulaC18H19N5O
Cas No.1200129-48-1
SmilesN#CC1=NC=C2NC=3N=CC=CC3C2=C1OC4CCN(CC)CC4
Storage & Solubility Information
Storagestore 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
H2O: 20 mg/mL (62.23 mM), when pH is adjusted to 3 with HCl. Sonication is recommmended.
Solution Preparation Table
H2O
1mg5mg10mg50mg
1 mM3.1116 mL15.5579 mL31.1158 mL155.5791 mL
5 mM0.6223 mL3.1116 mL6.2232 mL31.1158 mL
10 mM0.3112 mL1.5558 mL3.1116 mL15.5579 mL
20 mM0.1556 mL0.7779 mL1.5558 mL7.7790 mL
50 mM0.0622 mL0.3112 mL0.6223 mL3.1116 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:
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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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