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L-779,450
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。
L-779,450图片
CAS NO:303727-31-3
规格:98%
分子量:347.8
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
Raf kinase inhibitor
CAS:303727-31-3
分子式:C20H14ClN3O
分子量:347.8
纯度:98%
存储:Store at -20°C

Background:

L-779450 is a potent and selective B-Raf kinase inhibitor with a Kd of 2.4 nM.


L-779450 (L-779,450) shows a high degree of specificity towards Raf. The only other tested kinase inhibited is p38MAPK, which has a kinase domain structurally related to Raf. L-779450 inhibits anchorage-independent growth of human tumor lines at doses ranging from 0.3 to 2?μM[2]. The effects of L-779450 (L-779,450) on TRAIL sensitivity are investigated here in melanoma cell lines with high TRAIL sensitivity (A-375 and SK-Mel-147), moderate sensitivity (Mel-HO, SK-Mel-13, and SK-Mel-28), and permanent resistance (MeWo, Mel-2a, and SK-Mel-103), as well as in TRAIL-selected cell lines with acquired resistance (A-375-TS and Mel-HO-TS). Despite only moderate direct effects of L-779450 on apoptosis, it strongly enhances TRAIL-induced apoptosis in sensitive melanoma cells and overrules TRAIL resistance in Mel-2a, SK-Mel-103, A-375-TS, and Mel-HO-TS. At 24?hours, 16-35% apoptosis induction is obtained[3].


参考文献:
[1]. Takle AK, et al. The identification of potent, selective and CNS penetrant furan-based inhibitors of B-Raf kinase. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4373-6.
[2]. Shelton JG, et al. Differential effects of kinase cascade inhibitors on neoplastic and cytokine-mediated cell proliferation. Leukemia. 2003 Sep;17(9):1765-82.
[3]. Berger A, et al. RAF inhibition overcomes resistance to TRAIL-induced apoptosis in melanoma cells. J Invest Dermatol. 2014 Feb;134(2):430-440.