ML-18
目录号 : GC33152
A BB3 receptor antagonist
Cas No.:1422269-30-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment: | 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]. |
Cell experiment: | 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]. |
References: [1]. Moody TW, et al. ML-18 is a non-peptide bombesin receptor subtype-3 antagonist which inhibits lung cancer growth. Peptides. 2015 Feb;64:55-61. | |
ML-18 is a non-peptide bombesin receptor subtype 3 (BB3) antagonist that inhibits [125I]BA1 binding to NCI-H1299 lung cancer cells transfected with human BB3 receptors (IC50 = 4.8 μM).1 It is selective for BB3 over the gastrin releasing peptide receptor (GRPR) and the neuromedin B receptor (NMBR) with IC50 values of 16 and >100 μM, respectively, in a radioligand binding assay. ML-18 (16 μM) reversibly inhibits BA1-induced increases in cytosolic calcium in NCI-H1299 cells. It also inhibits BA1-induced phosphorylation of ERK and EGFR and reduces proliferation of NCI-H1299 cells.
1.Moody, T.W., Mantey, S.A., Moreno, P., et al.ML-18 is a non-peptide bombesin receptor subtype-3 antagonist which inhibits lung cancer growthPeptides6455-61(2015)
| Cas No. | 1422269-30-4 | SDF | |
| Canonical SMILES | O=C([C@@H](NC(NC1=CC=C(N(=O)=O)C=C1)=O)CC2=CNC3=CC=CC=C23)NCC4(C5=CC=C(OC)C=C5)CCCCC4 | ||
| 分子式 | C32H35N5O5 | 分子量 | 569.65 |
| 溶解度 | DMSO : ≥ 100 mg/mL (175.55 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。