GDC-0425 (RG-7602) 是一种有效的、具有口服活性的、高选择性的ChK1抑制剂。GDC-0425 可用于多种恶性肿瘤的研究。
| 生物活性 | GDC-0425 (RG-7602) is an orally available, highly selective small moleculeChK1inhibitor. GDC-0425 can be used for the research of various malignancies[1][2]. |
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体外研究
(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. |
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体内研究
(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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: H2O : 25 mg/mL(77.79 mM;ultrasonic and adjust pH to 3 with HCl) 配制储备液 | 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
