2. GDC-0425

GDC-0425 (RG-7602) is an orally available, highly selective small molecule ChK1 inhibitor. GDC-0425 can be used for the research of various malignancies.

For research use only. We do not sell to patients.

GDC-0425 Chemical Structure

GDC-0425 Chemical Structure

CAS No. : 1200129-48-1

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10 mg USD 110 In-stock
25 mg USD 220 In-stock
50 mg USD 380 In-stock
100 mg USD 600 In-stock
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GDC-0425 Related Antibodies

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Description

GDC-0425 (RG-7602) is an orally available, highly selective small molecule ChK1 inhibitor. GDC-0425 can be used for the research of various malignancies[1][2].

In Vitro

MEK inhibition either by pharmacologic inhibitors or RNAi-mediated gene silencing significantly protected cells from reduced viability upon GDC-0425 treatment[3].
GDC-0425 (3 μM; 24 hours) treatment results the hyperphosphorylation of Chk1[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GDC-0425 Related Antibodies

Cell Viability Assay[3]

Cell Line: Chk1-positive breast cancer cell lines
Concentration: 0.001, 0.01, 0.1, 1, 10 mM
Incubation Time: 72 hours
Result: Reduced cell proliferation.

Cell Viability Assay[3]

Cell Line: U-2 OS cells
Concentration: 3 μM
Incubation Time: 24 hours
Result: Led to hyperphosphorylation of Chk1.
In Vivo

GDC-0425 exhibits partial suppression of tumor growth. The Gemcitabine/GDC-0425 combination results in significant tumor regression in all tested models[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NCr nude mice bearing xenografts of both osteosarcoma and triple-negative breast cancer models (143B PML BK TK, HCC1806, and HCC70 cell lines)[3]
Dosage: For the 4-arm study, mice were treated with vehicle, Gemcitabine 120 mg/kg, GDC-0425 75 mg/kg alone, or Gemcitabine and GDC-0425 combination for 15 days. For 6-arm studies of HCC1806 and HCC70 models, mice were treated with vehicle, Gemcitabine 120 mg/kg, GDC-0425 50 mg/kg, GDC-0425 75 mg/kg alone, or Gemcitabine and GDC-0425 combination.
Administration: Orally administrated at 24, 48, and 72 hours after gemcitabine administration by intraperitoneal injection.
Result: Exhibited partial suppression of tumor growth upon treatment with either Gemcitabine or GDC-0425 alone. Notably, the Gemcitabine/GDC-0425 combination resulted in significant tumor regression in all tested models.
Clinical Trial
Molecular Weight

321.38

Formula

C18H19N5O
CAS No.
Appearance

Solid

Color

Off-white to brown

SMILES

N#CC1=NC=C2C(C3=CC=CN=C3N2)=C1OC4CCN(CC)CC4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 25 mg/mL (77.79 mM; ultrasonic and adjust pH to 3 with HCl)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1116 mL 15.5579 mL 31.1158 mL
5 mM 0.6223 mL 3.1116 mL 6.2232 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 3.1116 mL 15.5579 mL 31.1158 mL 77.7895 mL
5 mM 0.6223 mL 3.1116 mL 6.2232 mL 15.5579 mL
10 mM 0.3112 mL 1.5558 mL 3.1116 mL 7.7790 mL
15 mM 0.2074 mL 1.0372 mL 2.0744 mL 5.1860 mL
20 mM 0.1556 mL 0.7779 mL 1.5558 mL 3.8895 mL
25 mM 0.1245 mL 0.6223 mL 1.2446 mL 3.1116 mL
30 mM 0.1037 mL 0.5186 mL 1.0372 mL 2.5930 mL
40 mM 0.0778 mL 0.3889 mL 0.7779 mL 1.9447 mL
50 mM 0.0622 mL 0.3112 mL 0.6223 mL 1.5558 mL
60 mM 0.0519 mL 0.2593 mL 0.5186 mL 1.2965 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GDC-04251200129-48-1RG-7602GDC0425GDC 0425RG7602RG 7602Inhibitorinhibitorinhibit

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