1. GPCR/G Protein
  2. Bombesin Receptor
  3. ML-18

ML-18 

Cat. No.: HY-101844 Purity: 98.04%
Handling Instructions

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

For research use only. We do not sell to patients.

ML-18 Chemical Structure

ML-18 Chemical Structure

CAS No. : 1422269-30-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 226 In-stock
Estimated Time of Arrival: December 31
1 mg USD 50 In-stock
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5 mg USD 180 In-stock
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10 mg USD 250 In-stock
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25 mg USD 550 In-stock
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50 mg USD 950 In-stock
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100 mg USD 1200 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target

IC50: 4.8 μM (BRS-3)[1]

In Vitro

ML-18 inhibits specific 125I-BA1 (DTyr-Gln-Trp-Ala-Val-βAla-His-Phe-Nle-NH2)BB6-14 binding to NCI-H1299 lung cancer cells stably transfected with BRS-3 with IC50 values of 4.8 μM. ML-18 binds with lower affinity to the GRPR and NMBR with IC50 values of 16 and more than 100 μM, respectively. ML-18 at 16 μM inhibits the ability of 10 nM BA1 to elevate cytosolic Ca2+ in a reversible manner using lung cancer cells loaded with FURA2-AM. ML-18 at 16 μM inhibits the ability of 100 nM BA1 to cause tyrosine phosphorylation of the EGFR and ERK in lung cancer cells. It inhibits the proliferation of lung cancer cells[1].

Molecular Weight

569.65

Formula

C₃₂H₃₅N₅O₅

CAS No.

1422269-30-4

SMILES

O=C([[email protected]@H](NC(NC1=CC=C(N(=O)=O)C=C1)=O)CC2=CNC3=CC=CC=C23)NCC4(C5=CC=C(OC)C=C5)CCCCC4

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (175.55 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7555 mL 8.7773 mL 17.5546 mL
5 mM 0.3511 mL 1.7555 mL 3.5109 mL
10 mM 0.1755 mL 0.8777 mL 1.7555 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

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[1].

MCE has not independently confirmed the accuracy of these methods. 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 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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ML-18
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HY-101844
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