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ML-18

Catalog No. T4540Cas No. 1422269-30-4

ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 [mu]M.

ML-18

ML-18

Purity: 100%
Catalog No. T4540Cas No. 1422269-30-4
ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 [mu]M.
Pack SizePriceAvailabilityQuantity
1 mg$30In Stock
5 mg$58In Stock
10 mg$93In Stock
25 mg$188In Stock
50 mg$293In Stock
100 mg$473In Stock
200 mg$653In Stock
1 mL x 10 mM (in DMSO)$73In Stock
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Purity:100%
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Product Introduction

Bioactivity
Description
ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 [mu]M.
Targets&IC50
BRS3:4.8 μM.
In vitro
ML-18, at a concentration of 16 µM, reversibly inhibits BA1 at 10 nM from increasing cytosolic Ca2+ levels and at 100 nM from inducing tyrosine phosphorylation of EGFR and ERK in lung cancer cells, using FURA2-AM-loaded lung cancer cells for the former evaluation. This compound also suppresses lung cancer cell proliferation. Furthermore, ML-18 demonstrates specific inhibition of 125I-BA1 (DTyr-Gln-Trp-Ala-Val-βAla-His-Phe-Nle-NH2)BB6-14 binding to BRS-3-expressing NCI-H1299 lung cancer cells, presenting an IC50 value of 4.8 µM. It exhibits reduced affinity towards GRPR and NMBR with IC50 values of 16 µM and over 100 µM, respectively.
Kinase Assay
The cells are incubated in SIT buffer containing 0.25% bovine serum albumin and 250 μg/mL bacitracin and 125I-BA1 (100,000 cpm) is added, as well as various concentrations of unlabelled competitor (ML-18). After incubation at 37°C for 30 min, free 125I-BA1 is removed by washing 3 times in buffer and the cells which contain bound 125I-BA1 is dissolved in 0.2 N NaOH and counted in a gamma counter. The IC50 is calculated for each unlabeled competitor.
Cell Research
ML-18 is dissolved in DMSO at a concentration of 10 mM prior to use. Cell viability is measured using the MTT assay. NCI-H727 or NCI-H1299 cells transfected with BRS-3 are treated with ML-18 (0, 4.8, 16, 48 μM) or gefitinib added. After 2 days, 15 μL of 0.1 % MTT solution added. After 4 h, 150 μL of DMSO is added. After 16 h, the optical density at 570 nm is determined.
Chemical Properties
Molecular Weight569.65
FormulaC32H35N5O5
Cas No.1422269-30-4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (87.77 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.7555 mL8.7773 mL17.5546 mL87.7732 mL
5 mM0.3511 mL1.7555 mL3.5109 mL17.5546 mL
10 mM0.1755 mL0.8777 mL1.7555 mL8.7773 mL
20 mM0.0878 mL0.4389 mL0.8777 mL4.3887 mL
50 mM0.0351 mL0.1755 mL0.3511 mL1.7555 mL

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