1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEML-18Cat. No.: HY-101844CAS No.: 1422269-30-4分式: CHNO分量: 569.65作靶點(diǎn): Bombesin Receptor作通路: GPCR/G Protein儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (175.55 mM)* means soluble,

2、 but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.7555 mL 8.7773 mL 17.5546 mL5 mM 0.3511 mL 1.7555 mL 3.5109 mL10 mM 0.1755 mL 0.8777 mL 1.7555 mL請根據(jù)產(chǎn)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。BIOLOGICAL ACTIVITY物活性 ML-18種抑制肺癌長的肽鈴蟾肽受體亞型-3 (BRS-3) 拮抗劑。IC50 & Target IC50: 4.8

3、M (BRS-3) 1體外研究ML-18 inhibits specific 125I-BA1 (DTyr-Gln-Trp-Ala-Val-Ala-His-Phe-Nle-NH2)BB6-14 binding to NCI-H1299lung cancer cells stably transfected with BRS-3 with IC50 values of 4.8 M. ML-18 binds with lower affinity to1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEthe GRPR and NMBR with IC

4、50 values of 16 and more than 100 M, respectively. ML-18 at 16 M inhibitsthe ability of 10 nM BA1 to elevate cytosolic Ca2+ in a reversible manner using lung cancer cells loaded withFURA2-AM. ML-18 at 16 M inhibits the ability of 100 nM BA1 to cause tyrosine phosphorylation of theEGFR and ERK in lun

5、g cancer cells. It inhibits the proliferation of lung cancer cells 1.PROTOCOLKinase Assay 1 The cells are incubated in SIT buffer containing 0.25% bovine serum albumin and 250 g/mL bacitracin and125I-BA1 (100,000 cpm) is added, as well as various concentrations of unlabelled competitor (ML-18). Afte

6、rincubation at 37C for 30 min, free 125I-BA1 is removed by washing 3 times in buffer and the cells whichcontain bound 125I-BA1 is dissolved in 0.2 N NaOH and counted in a gamma counter. The IC50 is calculatedfor each unlabeled competitor 1.MCE has not independently confirmed the accuracy of these me

7、thods. They are for reference only.Cell Assay 1 Cell viability is measured using the MTT assay. NCI-H727 or NCI-H1299 cells transfected with BRS-3 aretreated with ML-18 (0, 4.8, 16, 48 M) or gefitinib added. After 2 days, 15 L of 0.1 % MTT solution added.After 4 h, 150 L of DMSO is added. After 16 h

8、, the optical density at 570 nm is determined 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Moody TW, et al. ML-18 is a non-peptide bombesin receptor subtype-3 antagonist which inhibits lung cancer growth. Peptides. 2015Feb;64:55-61.McePdfHeightCaution: Product has not been fully validated for medical applications