1、鵌缀(省搀%棰省冝省省讀缁缀谀耀螏頀h琀椀异缃缃缃弗猗笗笗笗刀洀吀伀刀攀渀栀椀戀椀琀漀爀攀搀栀攀洀砀瀀爀攀猀猀瀀搀昀瀀椀挀最椀昀刀洀吀伀刀攀渀栀椀戀椀琀漀爀攀搀栀攀洀砀瀀爀攀猀猀瀀搀昀尀尀攀昀挀挀戀昀昀昀戀攀昀愀洀欀愀渀夀漀渀琀攀夀栀戀堀椀猀爀倀稀瘀唀礀砀刀昀眀刀洀吀伀刀攀渀栀椀戀椀琀漀爀攀搀栀攀洀砀瀀爀攀猀猀攀挀攀愀昀攀挀昀攀搀昀搀挀愀刀愀琀一漀夀脀蜠脀萠氀舀一茀传匀尀摏瘯洀吀伀刀尀摏倀欀琀洀吀伀刀塐瀀爀漀琀攀挀琀昀爀漀洀氀椀最栀琀灠湥卣鹙豛匀伀洀最洀洀一攀攀搀甀氀琀爀愀猀漀渀椀挀伀最琀倀最琀最琀吀眀攀攀渀最琀最琀猀愀氀椀渀攀匀漀氀甀戀椀氀椀琀礀攀洀最洀洀氀攀愀爀猀漀氀甀琀椀漀渀鶋轏匀伀最琀
2、最琀挀漀爀渀漀椀氀匀漀氀甀戀椀氀椀琀礀攀洀最洀洀氀攀愀爀猀漀氀甀琀椀漀渀伀伀吀嘀吀夀挀椯刀f洀吀伀刀鄀刀刀椀挀琀漀爀洀吀伀刀吀協椀鄀洀吀伀刀刀眀靧扙萀嬀崀蔀耠栀漀甀爀猀栀愀猀最漀漀搀愀渀琀椀瀀爀漀瀀攀爀琀椀攀猀戀氀漀挀欀猀洀吀伀刀猀椀最渀愀氀椀渀最愀渀搀刀椀挀琀漀爀愀猀猀漀挀椀愀琀椀漀渀眀椀琀栀洀吀伀刀嬀崀刀栀漀甀爀猀搀椀猀瀀氀愀礀猀琀栀攀氀攀愀猀琀琀漀砀椀挀椀琀礀琀漀渀漀爀洀愀氀渀攀甀爀漀渀猀眀椀琀栀渀漀猀椀最渀椀昀椀挀愀渀琀挀礀琀漀琀漀砀椀挀攀昀昀攀挀琀猀昀漀爀挀漀渀挀攀渀琀爀愀琀椀漀渀猀甀瀀琀漀洀挀漀洀瀀愀爀攀搀琀漀嬀崀匀癸偺爀漀搀甀挀琀愀琀愀匀栀攀攀琀渀栀椀戀椀琀漀爀猀最漀渀椀猀琀猀匠
3、挀爀攀攀渀椀渀最椀戀爀愀爀椀攀猀眀眀眀攀搀栀攀洀砀瀀爀攀猀猀挀渀瀀漀瀀琀漀猀椀猀渀愀氀礀猀椀猀嬀崀攀氀氀椀渀攀唀挀攀氀氀猀一挀攀氀氀猀漀渀挀攀渀琀爀愀琀椀漀渀渀挀甀戀愀琀椀漀渀吀椀洀攀栀漀甀爀猀刀攀猀甀氀琀愀搀最漀漀搀愀渀琀椀瀀爀漀瀀攀爀琀椀攀猀愀渀搀戀氀漀挀欀攀搀洀吀伀刀猀椀最渀愀氀椀渀最愀渀搀刀椀挀琀漀爀愀猀猀漀挀椀愀琀椀漀渀眀椀琀栀洀吀伀刀攀氀氀礀琀漀琀漀砀椀挀椀琀礀猀猀愀礀嬀崀攀氀氀椀渀攀一漀爀洀愀氀洀愀琀甀爀攀栀甀洀愀渀渀攀甀爀漀渀猀漀渀挀攀渀琀爀愀琀椀漀渀渀挀甀戀愀琀椀漀渀吀椀洀攀栀漀甀爀猀刀攀猀甀氀琀椀猀瀀氀愀礀攀搀琀栀攀氀攀愀猀琀琀漀砀椀挀椀琀礀琀漀渀漀爀洀愀氀渀攀甀爀漀渀猀眀
4、椀琀栀渀漀猀椀最渀椀昀椀挀愀渀琀挀礀琀漀琀漀砀椀挀攀昀昀攀挀琀猀昀漀爀挀漀渀挀攀渀琀爀愀琀椀漀渀猀甀瀀琀漀洀匀蕏癸椀挀攀爀攀挀攀椀瘀椀渀最刀洀最欀最搀愀椀氀礀椀瀀昀漀爀搀愀礀猀洀最欀最搀愀椀氀礀椀瀀昀漀爀搀愀礀猀愀琀攀椀琀栀攀爀搀漀猀椀渀最爀攀最椀洀攀渀搀椀猀瀀氀愀礀洀愀爀欀攀搀椀渀栀椀戀椀琀椀漀渀漀昀琀甀洀漀爀最爀漀眀琀栀爀愀琀攀刀愀琀洀最欀最搀椀渀栀椀戀椀琀椀漀渀愀琀攀渀搀漀昀搀漀猀椀渀最瀀攀爀椀漀搀琀甀洀漀爀最爀漀眀琀栀搀攀氀愀礀搀愀礀猀刀愀琀洀最欀最搀椀渀栀椀戀椀琀椀漀渀愀琀攀渀搀漀昀搀漀猀椀渀最瀀攀爀椀漀搀琀甀洀漀爀最爀漀眀琀栀搀攀氀愀礀搀愀礀猀愀猀挀漀洀瀀愀爀攀搀琀漀洀椀挀攀爀攀挀
5、攀椀瘀椀渀最瘀攀栀椀挀氀攀愀氀漀渀攀嬀崀渀椀洀愀氀漀搀攀氀一挀攀氀氀猀椀渀昀攀洀愀氀攀猀挀椀搀吀愀挀漀渀椀挀洀椀挀攀嬀崀漀猀愀最攀洀最欀最洀最欀最搀洀椀渀椀猀琀爀愀琀椀漀渀愀椀氀礀椀瀀搀愀礀猀刀攀猀甀氀琀椀琀栀攀爀搀漀猀椀渀最爀攀最椀洀攀渀搀椀猀瀀氀愀礀攀搀洀愀爀欀攀搀椀渀栀椀戀椀琀椀漀渀漀昀琀甀洀漀爀最爀漀眀琀栀爀愀琀攀愀猀挀漀洀瀀愀爀攀搀琀漀洀椀挀攀爀攀挀攀椀瘀椀渀最瘀攀栀椀挀氀攀愀氀漀渀攀刀刀一匀嬀崀攀渀愀瘀椀搀攀猀匀攀爀爀愀琀漀攀琀愀氀匀瀀攀挀椀昀椀挀戀氀漀挀欀愀搀攀漀昀刀椀挀琀漀爀洀吀伀刀愀猀猀漀挀椀愀琀椀漀渀椀渀栀椀戀椀琀猀洀吀伀刀愀挀琀椀瘀椀琀礀愀渀搀椀猀挀礀琀漀琀漀砀椀挀椀渀最
6、氀椀漀戀氀愀猀琀漀洀愀倀漀匀伀渀攀瀀爀攀挀攀倀搀昀攀椀最栀琀愀甀琀椀漀渀倀爀漀搀甀挀琀栀愀猀渀漀琀戀攀攀渀昀甀氀氀礀瘀愀氀椀搀愀琀攀搀昀漀爀洀攀搀椀挀愀氀愀瀀瀀氀椀挀愀琀椀漀渀猀漀爀爀攀猀攀愀爀挀栀甀猀攀漀渀氀礀吀攀氀愀砀洀愀椀氀琀攀挀栀攀搀栀攀洀砀瀀爀攀猀猀挀渀愀猀琀攀爀漀昀匀洀愀氀氀漀氀攀挀甀氀攀猀鵠蒏酶睞眀眀攀搀栀攀洀砀瀀爀攀猀猀挀渀攀搀栀攀洀砀瀀爀攀猀猀靓de mice aged 6-8 weeks. Tumor volumes are calculated. Ten mice with the appropriate mean tumor volume are assigned ra
7、ndomLy to each of six groups. The mean tumor volumethe standard error of the mean (SEM) for all six groups is 1683 mm3 at the initiation of treatment (Day 0). Mice are dosed 1 or vehicle (PBS) by oral gavage with a dose volume of 4.0 mL/kg. The mice are observed on each day of the study, and tumor v
8、olumes and body weights are measured twice each week. Percent tumor growth inhibition is calculated using the formula %TGI=100 (1- Tumor Volumedose/Tumor Volumevehicle).MCE has not independently confirmed the accuracy of these methods. They are for reference only.客户使本产品发表的科研献 Sci Signal. 2018 Jul 17
9、;11(539). pii: eaao3964.www.MedChemE2See more customer validations on www.MedChemEREFERENCES1. Flygare JA, et al. Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treat鹸(省搀儀棵省砂冞省省讀缁缀耀螏頀h椀鼃弄洄洍洍褍鴍愀渀猀漀瀀爀愀稀漀氀攀猀漀搀椀甀洀猀漀搀椀甀洀倀爀漀琀漀渀倀甀洀瀀渀栀
10、椀戀椀琀漀爀攀搀栀攀洀砀瀀爀攀猀猀瀀搀昀瀀椀挀最椀昀愀渀猀漀瀀爀愀稀漀氀攀猀漀搀椀甀洀猀漀搀椀甀洀倀爀漀琀漀渀倀甀洀瀀渀栀椀戀椀琀漀爀攀搀栀攀洀砀瀀爀攀猀猀瀀搀昀尀尀挀搀愀昀挀戀挀戀挀昀栀砀戀圀砀眀樀堀搀洀堀匀樀匀最攀甀琀眀戀匀栀渀娀焀琀匀吀圀氀焀吀樀洀焀愀礀愀渀猀漀瀀爀愀稀漀氀攀猀漀搀椀甀洀倀爀漀琀漀渀倀甀洀瀀渀栀椀戀椀琀漀爀攀搀栀攀洀砀瀀爀攀猀猀搀攀挀搀昀昀昀戀昀愀戀愀渀猀漀瀀爀愀稀漀氀攀猀漀搀椀甀洀愀琀一漀夀匀一漀脀蘠脀茠茀丠茀丠愀伀舀匠尀摏瘯倀爀漀琀漀渀倀甀洀瀀尀摏攀洀戀爀愀渀攀吀爀愀渀猀瀀漀爀琀攀爀漀渀栀愀渀渀攀氀塐倀氀攀愀猀攀猀琀漀爀攀琀栀攀瀀爀漀搀甀挀琀甀渀搀攀爀琀栀攀爀攀挀漀洀
11、洀攀渀搀攀搀挀漀渀搀椀琀椀漀渀猀椀渀琀栀攀伀伀伀吀嘀吀夀挀椯愀渀猀漀瀀爀愀稀漀氀攀酬醀碀掑到刀一匀嬀崀漀欀甀昀甀吀攀琀愀氀昀昀攀挀琀猀漀昀氀愀渀猀漀瀀爀愀稀漀氀攀漀渀瀀栀愀爀洀愀挀漀欀椀渀攀琀椀挀猀愀渀搀洀攀琀愀戀漀氀椀猀洀漀昀琀栀攀漀瀀栀礀氀氀椀渀攀甀爀氀椀渀倀栀愀爀洀愀挀漀氀瀀嬀崀愀椀攀琀愀氀愀渀猀漀瀀爀愀稀漀氀攀昀漀爀琀栀攀瀀爀攀瘀攀渀琀椀漀渀漀昀爀攀挀甀爀爀攀渀挀攀猀漀昀甀氀挀攀爀挀漀洀瀀氀椀挀愀琀椀漀渀猀昀爀漀洀氀漀渀最琀攀爀洀氀漀眀搀漀猀攀愀猀瀀椀爀椀渀甀猀攀一渀最氀攀搀瀀嬀崀眀愀栀椀吀攀琀愀氀愀渀猀漀瀀爀愀稀漀氀攀愀渀漀瘀攀氀戀攀渀稀椀洀椀搀愀稀漀氀攀瀀爀漀琀漀渀瀀甀洀瀀椀渀栀椀
12、戀椀琀漀爀愀渀搀椀琀猀爀攀氀愀琀攀搀挀漀洀瀀漀甀渀搀猀栀愀瘀攀猀攀氀攀挀琀椀瘀攀愀挀琀椀瘀椀琀礀愀最愀椀渀猀琀攀氀椀挀漀戀愀挀琀攀爀瀀礀氀漀爀椀渀琀椀洀椀挀爀漀戀最攀渀琀猀栀攀洀漀琀栀攀爀瀀挀攀倀搀昀攀椀最栀琀愀甀琀椀漀渀倀爀漀搀甀挀琀栀愀猀渀漀琀戀攀攀渀昀甀氀氀礀瘀愀氀椀搀愀琀攀搀昀漀爀洀攀搀椀挀愀氀愀瀀瀀氀椀挀愀琀椀漀渀猀漀爀爀攀猀攀愀爀挀栀甀猀攀漀渀氀礀吀攀氀愀砀洀愀椀氀琀攀挀栀攀搀栀攀洀砀瀀爀攀猀猀挀渀愀猀琀攀爀漀昀匀洀愀氀氀漀氀攀挀甀氀攀猀鵠蒏酶偞爀漀搀甀挀琀愀琀愀匀栀攀攀琀渀栀椀戀椀琀漀爀猀最漀渀椀猀琀猀匠挀爀攀攀渀椀渀最椀戀爀愀爀椀攀猀眀眀眀攀搀栀攀洀砀瀀爀攀猀猀挀渀攀搀栀攀洀砀
13、瀀爀攀猀猀靓欁言茀渀7砀冞省岨:退鄀鹸胔-)輀.棙i缀$Lck-Inhibitor-Src-Inhibitor-MedChemExpress.pdfpic1.gifLckInhibitorSrcInhibitorMedChemExpress.pdf2019-625eb1c1a99-8233-42e2-b8de-5e4e7571d04fYcRm4C+tgiQnOjlTFfWpstCioWeY8AaGf97hwv15IdiSLft/MSXFtw=Lck,Inhibitor,Src,MedChemExpress7e5ce5e585ea21117b08f170dc89d0abLck Inhibitor
14、Cat. No.: HY-12072CAS No.: 847950-09-8分式: CHNO分量: 530.62作靶点: Src作通路: Protein Tyrosine Kinase/RTK储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (188.46 mM; Need ultrasonic)ConcentrationSolvent Mass 1 mg 5 mg 10 mg1 mM 1.8846 mL 9.4229 mL 18.8459 mL5 m
15、M 0.3769 mL 1.8846 mL 3.7692 mL制备储备液10 mM 0.1885 mL 0.9423 mL 1.8846 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液体内实验 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.71 mM); Clear solution1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.71 mM); Clear solution2. BIOLOGICAL
16、ACTIVITY物活性 Lck Inhibitor是新型的 Lck抑制剂， IC50为7 nM。REFERENCES1. Martin, Matthew W.; Newcomb, John; Nunes, Joseph J.; et al. Structure-Based Design of Novel 2-Amino-6-phenyl-pyrimido5,4:5,6pyrimido1,2-abenzimidazol-5(6H)-ones as Potent and Orally Active Inhibitors of Lymphocyte Specific Kinase (Lck): Sy
17、nthesis, SAR, and In Vivo Anti-Inflammatory Activity. Journal of Medicinal Chemistry (2008), 51(6), 1637-1648.Product Data Sheet InhibitorsAgonistsScreening Librarieswww.MedChemE12. Liew, Chin Y.; Ma, Xiao H.; Liu, Xianghui; Yap, Chun W. SVM Model for Virtual Screening of Lck Inhibitors. Journal of
18、Chemical Information and Modeling (2009), 49(4), 877-885.McePdfHeightCaution: Product has not been fully validated for medical applications. For research use only.Tel: 400-820-3792; 021-58955995 Fax: 021-53700325 E-mail: techMedChemEMaster of Small Molecules 您边的抑制剂师www.MedChemE2MedChemExpress0001500
19、006先进医疗20190625152405444351L挀瀀栀琀洀氀篨省/Ic前台访问/p-22999.html207.46.13.2420俤挀瀀栀琀洀氀篨蠀省夀/Ic前台访问/p-32886.html157.55.39.1320跐最瀀栀琀洀氀篨省婭/G_前台访问/p-9630.html54.36.148.570最瀀栀琀洀氀篨怀省帀/Ig前台访问/d-17386.html120.236.174.1600黖愀瀀栀琀洀氀篨悷省焍/Ke前台访问/p-422160.html10.124.145.260开椀栀琀洀氀篨舀悷省/Kg前台访问/p-422160.html119.123.32.1780淐最瀀栀琀洀氀篨怀珠省踀/Ie前台访问/d-13663.html46.229.168.1310%錀猀攀愀爀挀栀栀琀洀氀瀀愀洀瀀焀篨省孍/Ga前台访问/p-5676.html203.208.60.590朧攀瀀栀琀洀氀篨省/Kc前台访问/p-320462.html54.36.148.810椀瀀
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