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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。
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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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 263 | 现货 | |
5 mg | ¥ 530 | 现货 | |
10 mg | ¥ 833 | 现货 | |
25 mg | ¥ 1,690 | 现货 | |
50 mg | ¥ 2,710 | 现货 | |
100 mg | ¥ 4,330 | 现货 | |
200 mg | ¥ 5,850 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 648 | 现货 |
产品描述 | ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 μM. |
靶点活性 | BRS3:4.8 μM. |
体外活性 | ML-18以16 μM浓度,通过使用加载了FURA2-AM的肺癌细胞,可可逆性地抑制10 nM BA1提高细胞内Ca2+的能力。相同浓度下,ML-18能够抑制100 nM BA1引起的肺癌细胞中EGFR和ERK的酪氨酸磷酸化,进而抑制肺癌细胞的增殖。此外,ML-18还具有抑制具体125I-BA1(DTyr-Gln-Trp-Ala-Val-βAla-His-Phe-Nle-NH2)BB6-14与稳定转染BRS-3的NCI-H1299肺癌细胞结合的能力,其IC50值为4.8 μM。而对GRPR和NMBR的亲和力较低,其IC50值分别为16 μM和超过100 μM。 |
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. |
分子量 | 569.65 |
分子式 | C32H35N5O5 |
CAS No. | 1422269-30-4 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (87.77 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
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