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ML-18
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ML-18图片
CAS NO:1422269-30-4
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
ML-18是一种非肽铃蟾肽受体亚型-3 拮抗剂,能够抑制肺癌生长。

产品描述

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

体外活性

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. 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.

激酶实验

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.

细胞实验

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.

Cas No.

1422269-30-4

分子式

C32H35N5O5

分子量

569.662

储存和溶解度

DMSO:100 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years