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