GDC-0425
Modify Date: 2024-01-14 17:48:32
GDC-0425 structure
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Common Name | GDC-0425 | ||
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| CAS Number | 1200129-48-1 | Molecular Weight | 321.38 | |
| Density | 1.3±0.1 g/cm3 | Boiling Point | 589.2±50.0 °C at 760 mmHg | |
| Molecular Formula | C18H19N5O | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 310.2±30.1 °C | |
Use of GDC-0425GDC-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]. |
| Name | 5-[(1-Ethyl-4-piperidinyl)oxy]-9H-pyrido[4',3':4,5]pyrrolo[2,3-b]pyridine-6-carbonitrile |
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| Synonym | More Synonyms |
| 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]. |
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| Related Catalog | |
| Target |
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]. 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]. 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. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 589.2±50.0 °C at 760 mmHg |
| Molecular Formula | C18H19N5O |
| Molecular Weight | 321.38 |
| Flash Point | 310.2±30.1 °C |
| Exact Mass | 321.158966 |
| LogP | 3.82 |
| Vapour Pressure | 0.0±1.7 mmHg at 25°C |
| Index of Refraction | 1.686 |
| 5-[(1-Ethyl-4-piperidinyl)oxy]-9H-pyrido[4',3':4,5]pyrrolo[2,3-b]pyridine-6-carbonitrile |
| 9H-Pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile, 5-[(1-ethyl-4-piperidinyl)oxy]- |