L-779450產(chǎn)品描述:L-779450 is a potent, ATP-competitive Raf kinase inhibitor (IC50 =10 nM) that displays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck respectively.IC50 value:Target: Raf inhibitorL-779450 suppressed DNA synthesis and induced apoptosis in hematopoietic FDC-P1 cells transformed to grow in response to either Raf-1 or A-Raf (FD/DeltaRaf-1:ER and FD/DeltaA-Raf:ER), but it displayed less effects on DNA synthesis and apoptosis when the cells were cultured in IL-3. L-779450 was less effective on B-Raf- or MEK1-responsive cells [1]. Treatment with L779450, but not PLX4720, induced strong KSR1/B-Raf binding in A549 and HMCB cells that possess oncogenic Ras proteins, in the Cal12T line that contains an impaired activity B-Raf mutant, and, surprisingly, in A375 melanoma cells that are homozygous for V600E-B-Raf. L779450-induced B-Raf/C-Raf dimerization was not reduced in MEFs expressing the R615H- and C809Y-KSR1 mutants unable to bind B-Raf; wheras B-Raf/C-Raf dimerization wa 公司介紹:MedChemExpress(MCE)專注于各種抑制劑、激動(dòng)劑、API及化合物庫,總部位于美國新澤西,分別在瑞典和上海設(shè)有歐洲區(qū)子公司和亞洲區(qū)總代理,營銷網(wǎng)點(diǎn)遍及全球20多個(gè)國家地區(qū)。MCE經(jīng)過多年努力已成為全球生物活性小分子領(lǐng)域的一流供應(yīng)商, 產(chǎn)品涵蓋癌癥、神經(jīng)科學(xué)、抗感染、表觀遺傳學(xué)等20個(gè)熱門研究領(lǐng)域,PI3K、MAPK等近千個(gè)細(xì)分靶點(diǎn),超過4000個(gè)活性小分子化合物現(xiàn)貨,以及GPCR、API、離子通道等超過20種不同類型的化合物庫,同時(shí)提供從毫克到千克的專業(yè)定制合成服務(wù)。 MCE 對(duì)每批產(chǎn)品都進(jìn)行嚴(yán)格的LCMS和NMR檢驗(yàn),其產(chǎn)品已被全球近萬名客戶廣泛使用并發(fā)表大量文章、專利; MCE 定期增加各領(lǐng)域熱門抑制劑、激動(dòng)劑,不斷擴(kuò)增已有化合物庫,以滿足最新的科研需求; 數(shù)千種產(chǎn)品在上海有充足備貨,24-48小時(shí)內(nèi)送達(dá)客戶; 大量產(chǎn)品提供免費(fèi)試用裝;已為全球多個(gè)知名企業(yè)、院校構(gòu)建各種定制型化合物庫。 產(chǎn)品鏈接:www.medchemexpress.cn/l-779450.html |
L-779450研究進(jìn)展
發(fā)布日期:2017-11-01 瀏覽次數(shù):0
核心提示:a href=https://www.medchemexpress.com/L-779450.htmlL-779450/a產(chǎn)品描述:L-779450 is a potent, ATP-competitive Raf kinase
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