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AZD8330
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AZD8330图片
CAS NO:869357-68-6
规格:98%
分子量:461.23
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
MEK 1/2 inhibitor
CAS:869357-68-6
分子式:C16H17FIN3O4
分子量:461.23
纯度:98%
存储:Store at -20°C

Background:

AZD8330 is an orally active and selective MEK1/2 inhibitor with an IC50 of 7 nM. The inhibition of MEK1/2 by this component results in inhibition of growth factor-mediated cell signaling and tumor cell proliferation.


MEK, also known as MAP kinase kinase (MAP2K), is a kinase enzyme which phosphorylates mitogen-activated protein kinase (MAPK). The activation of MAPK signaling pathway was shown to be involved in regulation of various cell processes including cell proliferation, differentiation, apoptosis, metabolism and inflammation.


AZD8330 treatment was shown to cause cell apoptosis by suppressing the activation of ERK1/2 signal transduction pathway in Burkitt's lymphoma cell line Raji cells, which is in a dose and time dependent manner [1].


Recently, a large phase I trial of 82 patients with advanced tumor malignancies was conducted to define the maximum tolerated dose (MTD) and assessed the safety, tolerability, pharmacokinetics and pharmacodynamics of AZD8330. The MTD of this product was determined as 40mg/day [2].


参考文献:
1.  Feng K, Wang C, Zhou H, Yang J, Dong L, Zhou K, et al. [Effect of ERK1/2 inhibitor AZD8330 on human Burkitt's lymphoma cell line Raji cells and its mechanism]. Zhonghua Xue Ye Xue Za Zhi 2015,36:148-152.
2.  Cohen RB, Aamdal S, Nyakas M, Cavallin M, Green D, Learoyd M, et al. A phase I dose-finding, safety and tolerability study of AZD8330 in patients with advanced malignancies. Eur J Cancer 2013,49:1521-1529.