1. Cell Cycle/DNA Damage
  2. Checkpoint Kinase (Chk)
  3. GDC-0425

GDC-0425 (Synonyms: RG-7602)

Cat. No.: HY-19926 Purity: 99.48%
Handling Instructions

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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5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 110 In-stock
Estimated Time of Arrival: December 31
25 mg USD 220 In-stock
Estimated Time of Arrival: December 31
50 mg USD 380 In-stock
Estimated Time of Arrival: December 31
100 mg USD 600 In-stock
Estimated Time of Arrival: December 31
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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].

IC50 & Target[1]

Chk1

 

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].

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

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].

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.
Molecular Weight

321.38

Formula

C₁₈H₁₉N₅O

CAS No.
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
10 mM 0.3112 mL 1.5558 mL 3.1116 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Product Name:
GDC-0425
Cat. No.:
HY-19926
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