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ML-18

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Purity:100%

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COA HNMR LCMS

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 μM.

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Pack Size	Price	Availability
1 mg	$47	In Stock
2 mg	$65	In Stock
5 mg	$97	In Stock
10 mg	$155	In Stock
25 mg	$313	In Stock
50 mg	$490	In Stock
100 mg	$788	In Stock
200 mg	$1,090	In Stock
500 mg	$1,620	In Stock
1 mL x 10 mM (in DMSO)	$122	In Stock

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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 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 Weight	569.65
Formula	C32H35N5O5
Cas No.	1422269-30-4

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (87.77 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.7555 mL	8.7773 mL	17.5546 mL	87.7732 mL
5 mM	0.3511 mL	1.7555 mL	3.5109 mL	17.5546 mL
10 mM	0.1755 mL	0.8777 mL	1.7555 mL	8.7773 mL
20 mM	0.0878 mL	0.4389 mL	0.8777 mL	4.3887 mL
50 mM	0.0351 mL	0.1755 mL	0.3511 mL	1.7555 mL

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