ML-18

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Chemical Structure| 1422269-30-4 同义名 : -
CAS号 : 1422269-30-4
货号 : A708758
分子式 : C32H35N5O5
纯度 : 98%+
分子量 : 569.651
MDL号 : MFCD30182327
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(184.32 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Bombesin receptor subtype (BRS)-3 is an orphan G-protein coupled receptor (GPCR) whose role in normal physiology is unknown due to a lack of specific agonists and antagonists. ML-18, an antagonist of BRS-3 with IC50 of 4.8 μM, is used to inhibit lung cancer growth. Addition of 16 μM ML-18 antagonized the ability of 10 nM BA1 to increase cytosolic Ca2+ in lung cancer cells. Subsequent addition of 1 μM BA1 increased the cytosolic Ca2+ strongly indicating that ML-18 is a reversible nonpeptide BRS-3 antagonist. The increase in FAK, ERK and EGFR tyrosine phosphorylation caused by 0.1 μM BA1 was significantly inhibited by 16 μM ML-18. The results indicate that ML-18 in a dose-dependent manner decreases lung cancer FAK, ERK and EGFR tyrosine phosphorylation that is regulated by BRS-3. Further, proliferation of NCI-H1299 cells transfected with BRS-3 was moderately and strongly inhibited by 16 and 48 μM ML-18. In the clonogenic assay, 1.6 μM ML-18 significantly reduced the NCI-H727 colony number. Finally, 10 nM MK5046 (BRS-3 agonist) stimulated and increase in cytosolic calcium of NCI-H1299 cells transfected with BRS-3 and this increase was inhibited by ML-18 at 16 μM[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.76mL

0.35mL

0.18mL

8.78mL

1.76mL

0.88mL

17.55mL

3.51mL

1.76mL
参考文献

[1]Moody TW, Mantey SA, Moreno P, et al. ML-18 is a non-peptide bombesin receptor subtype-3 antagonist which inhibits lung cancer growth. Peptides. 2015;64:55-61