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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.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $149 | - | In Stock |
| 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]. |
| Synonyms | RG-7602 |
| Molecular Weight | 321.38 |
| Formula | C18H19N5O |
| Cas No. | 1200129-48-1 |
| Smiles | N#CC1=NC=C2NC=3N=CC=CC3C2=C1OC4CCN(CC)CC4 |
| Storage | store 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
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Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
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
and mix thoroughly until a homogeneous solution is obtained.
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