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。
货号:ajcx34798
CAS:1200129-48-1
分子式:C18H19N5O
分子量：321.38
溶解度:H2O : 25 mg/mL (77.79 mM; ultrasonic and adjust pH to 3 with HCl)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

GDC-0425 exhibits partial suppression of tumor growth. The Gemcitabine/GDC-0425 combination results in significant tumor regression in all tested models[3].

[1]. Xiao Ding, et al. A supported liquid extraction LC-MS/MS method for determination of concentrations of GDC-0425, a small molecule Checkpoint kinase 1 inhibitor, in human plasma. Biomed Chromatogr. 2016 Dec;30(12):1984-1991.
[2]. Jeffrey R Infante, et al. Phase I Study of GDC-0425, a Checkpoint Kinase 1 Inhibitor, in Combination with Gemcitabine in Patients with Refractory Solid Tumors. Clin Cancer Res. 2017 May 15;23(10):2423-2432.
[3]. Ho-June Lee, et al. Ras-MEK Signaling Mediates a Critical Chk1-Dependent DNA Damage Response in Cancer Cells. Mol Cancer Ther. 2017 Apr;16(4):694-704.