



下載本文檔
版權說明:本文檔由用戶提供并上傳,收益歸屬內容提供方,若內容存在侵權,請進行舉報或認領
文檔簡介
1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAG 555Cat. No.: HY-15336CAS No.: 133550-34-2Synonyms: Tyrphostin AG 555分式: CHNO分量: 322.36作靶點: EGFR作通路: JAK/STAT Signaling; Protein Tyrosine Kinase/RTK儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實
2、驗 DMSO : 100 mg/mL (310.21 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.1021 mL 15.5106 mL 31.0212 mL5 mM 0.6204 mL 3.1021 mL 6.2042 mL10 mM 0.3102 mL 1.5511 mL 3.1021 mL請根據產品在不同溶劑中的溶解度,選擇合適的溶劑配制儲備液,并請注意儲備液的保存式和期限。體內實驗 請根據您的實驗動物和給藥式選擇適當的溶解案,配制前請先配制澄
3、清的儲備液,再依次添加助溶劑(為保證實驗結果的可靠性,體內實驗的作液,建議您現現配,當天使;澄清的儲備液可以根據儲存條件,適當保存;以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占):1. 請依序添加每種溶劑: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.76 mM); Clear solution2. 請依序添加每種溶劑: 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.76 mM); Clear solution1/2 Mast
4、er of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 AG 555種EGFR酪氨酸激酶抑制劑。IC50 & Target EGFR體外研究 The tyrosine kinase inhibitor (Tyrphostin) AG 555 selectively interferes with viral transcription in bovinepapillomavirus type 1 (BPV-1)-transformed fibroblasts and induces suppression of cycli
5、n-dependent kinaseactivity and cell cycle arrest. AG 555 treatment also leads to an activation of the mitogen-activated proteinkinase pathway by enhancing phosphorylation of JNK and p38. Tyrphostin AG 555 disturbs the balance ofnegative and positive regulatory factors necessary to maintain the homeo
6、stasis of a virus-transformedphenotype. Tyrphostin AG 555 can selectively suppress BPV-1 transcription through MAP kinase pathwayactivation and binding of phosphorylated Jun/ATF-2 at a novel intragenic regulatory sequence. AG 555affects the transcription of the major regulatory viral protein E2 by s
7、hifting the ratio between E2 transactivatorin favor to the repressor function. Cell incubation in the presence of 30 M AG 555 results in a selectivedown-regulation of the most abundant viral transcripts already 4 h after drug application 2. TyrphostinsAG555, which blocks Cdk2 activation, induces gro
8、wth arrest of immortalized cells at G1-S and early S and isvery effective in arresting the growth of EGFR overexpressor cells. AG55 inhibits the growth of HPV16-immortalized cells. AG555 is already effective at 10 M (IC50=6.4, respectively), and the cells remainarrested after withdrawal of the compo
9、und on day 5 as monitored on days 8 and 12 3.PROTOCOLCell Assay 2 ID13 mouse fibroblasts are maintained in Dulbeccos modified Eagles medium supplemented with 5% (v/v)fetal calf serum, 100 units/mL Penicillin, and 100 g/mL Streptomycin. Cells are seeded at 2.5104 cells/cm2to ensure logarithmic growth
10、. The final concentration of the Tyrphostin AG 555 is 30 M in all experiments.Stock solutions of 10 mM in Me2SO are stored at -80C. To exclude potential Me2SO effects, the same finalconcentrations (0.3%) of Me2SO are added to nontreated controls. Actinomycin D is dissolved in water andadded to cells
11、 in a final concentration of 5 g/mL. SB 203580 is dissolved in Me2SO (stock concentration: 50mM) and used in a final concentration of 10 M 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Michaelis M, et al. Cisplatin-resistant neuroblasto
12、ma cells express enhanced levels of epidermal growth factor receptor (EGFR) and aresensitive to treatment with EGFR-specific toxins. Clin Cancer Res. 2008 Oct 15;14(20):6531-7.2. Baars S, et al. Tyrphostin AG 555 inhibits bovine papillomavirus transcription by changing the ratio between E2 transactivator/repressorfunction. J Biol Chem. 2003 Sep 26;278(39):37306-13.3. Ben-Bassat H, et al. Tyrphostins that suppress the growth of human papilloma virus 16-immortalized human keratinocytes. J PharmacolExp Ther. 1999 Sep;290(3):1442-57.McePdfHeight2/2 Master of Small Molecules 您邊的抑制劑師www.MedC
溫馨提示
- 1. 本站所有資源如無特殊說明,都需要本地電腦安裝OFFICE2007和PDF閱讀器。圖紙軟件為CAD,CAXA,PROE,UG,SolidWorks等.壓縮文件請下載最新的WinRAR軟件解壓。
- 2. 本站的文檔不包含任何第三方提供的附件圖紙等,如果需要附件,請聯系上傳者。文件的所有權益歸上傳用戶所有。
- 3. 本站RAR壓縮包中若帶圖紙,網頁內容里面會有圖紙預覽,若沒有圖紙預覽就沒有圖紙。
- 4. 未經權益所有人同意不得將文件中的內容挪作商業或盈利用途。
- 5. 人人文庫網僅提供信息存儲空間,僅對用戶上傳內容的表現方式做保護處理,對用戶上傳分享的文檔內容本身不做任何修改或編輯,并不能對任何下載內容負責。
- 6. 下載文件中如有侵權或不適當內容,請與我們聯系,我們立即糾正。
- 7. 本站不保證下載資源的準確性、安全性和完整性, 同時也不承擔用戶因使用這些下載資源對自己和他人造成任何形式的傷害或損失。
最新文檔
- 北京市清華大學附中2025年化學高二下期末綜合測試試題含解析
- 江西省新余第四中學、上高第二中學2025屆高一化學第二學期期末聯考試題含解析
- 發票搖獎資金管理辦法
- 園區企業梯隊管理辦法
- 江蘇工地進度管理辦法
- 佛教用品規范管理辦法
- 農業公司戰略管理辦法
- 新疆煤礦礦井管理辦法
- 村民身份認定管理辦法
- 小學生經典古詩文誦讀活動
- 船廠安全用電培訓課件
- 《2025年CSCO腎癌診療指南》解讀
- 人教版九年級化學上冊暑假銜接講義(初二升初三)
- 跆拳道館技術崗位薪酬制度
- 無人駕駛車法規-深度研究
- 《寧晉縣國土空間總體規劃(2021-2035年)》
- 2024年度乳腺癌篩查與早期診斷課件
- 2024年食品檢驗員(高級)職業鑒定理論考試題庫(含答案)
- 工廠物品回收合同模板
- JJF 1168-2024便攜式制動性能測試儀校準規范
- 經橈動脈介入診療患者術肢并發癥預防及護理專家共識解讀
評論
0/150
提交評論