Hotline:400-820-3792
Inhibitors?ScreeningLibraries?Proteins
www.MedChemE
AMG410
Cat.No.:HY-173632
CASNo.:3040175-17-2
分?式:C??H??ClF?N?O?
分?量:656.08
作?靶点:Ras
作?通路:GPCR/GProtein;MAPK/ERKPathway
储存?式:Pleasestoretheproductundertherecommendedconditionsin
theCertificateofAnalysis.
BIOLOGICALACTIVITY
?物活性AMG410是?种?共价选择性泛KRAS抑制剂，对KRASG12D、KRASG12V和KRASG13D的IC50值为1-4
nM。AMG410对HRAS和NRAS的选择性均?于100倍。AMG410是?种GTP(开启)和GDP(关闭)状态的双
抑制剂(GDP状态的Kd值为1nM；GTP状态的Kd值为22nM）。AMG410能够以不依赖循环状态的?式阻
断KRAS信号传导，并抑制野?型KRAS扩增的肿瘤细胞增殖。AMG410可?于结直肠癌、胰腺癌和肺癌的研
究[1][2]。
IC50TargetKRasG12DKRasG12VKRASG13D
1-4nM(IC50)1-4nM(IC50)1-4nM(IC50)
REFERENCES
[1].AdrianoBAUER,etal.Macrocyclickrasinhibitorsandmethodsofuse.WO2024107686A1.
[2].ND01-AMG410:AnH/NRAS-sparingpan-KRASinhibitorwithdualGTP(on)/GDP(off)-stateactivityforthetreatmentofdiverseKRAS-
mutanttumors
McePdfHeight
Ca