GDC-0425 (Synonyms: RG-7602)
目录号: PL13953 纯度: ≥99%
CAS No. :1200129-48-1
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中文名称
GDC-0425
中文别名
5-((1-乙基哌啶-4-基)氧基)-9H-吡咯并[2,3-B:5,4-C']二吡啶-6-甲腈
英文名称
GDC-0425
英文别名
GDC-0425;5-((1-ethylpiperidin-4-yl)oxy)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile;5-(1-ethylpiperidin-4-yloxy)-9H-dipyrido[2,3-b-4',3'-d]pyrrole-6-carbonitrile;RG7602;RG-7602
Cas No.
1200129-48-1
分子式
C18H19N5O
分子量
321.38
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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 molecule ChK1 inhibitor. GDC-0425 can be used for the research of various malignancies.
性状
Solid
IC50 & Target[1][2]
Chk1
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.
GDC-0425 (3 μM; 24 hours) treatment results the hyperphosphorylation of Chk1. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay-tbl">
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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
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
ClinicalTrial
参考文献
[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.
溶解度数据
In Vitro: H2O : 25 mg/mL (77.79 mM; ultrasonic and adjust pH to 3 with HCl)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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