Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GDC-0425 (RG-7602) 是一种可口服的、高选择性的 ChK1抑制剂。GDC-0425 可用于多种恶性肿瘤的研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 347 | 5日内发货 | ||
5 mg | ¥ 578 | 5日内发货 | ||
10 mg | ¥ 1,090 | 5日内发货 |
产品描述 | GDC-0425 (RG-7602) is an orally administered, selective small molecule inhibitor targeting checkpoint kinase 1 (ChK1), utilized in research focused on various malignancies [1] [2]. |
体外活性 | Inhibition of MEK 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. |
体内活性 | GDC-0425 shows 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. |
分子量 | 321.38 |
分子式 | C18H19N5O |
CAS No. | 1200129-48-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
GDC-0425 1200129-48-1 GDC 0425 GDC0425 Inhibitor inhibitor inhibit