Powder: -20°C for 3 years | In solvent: -80°C for 1 year
NHWD-870 是一种有效且特异性的 BET 家族溴结构域抑制剂,仅与 BRD2、BRD3、BRD4 (IC50 = 2.7 nM) 和 BRDT 结合。 NHWD-870 具有强大的抗肿瘤功效,并通过增加肿瘤细胞凋亡和抑制肿瘤增殖来抑制癌细胞-巨噬细胞相互作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 2,980 | 5日内发货 | ||
25 mg | ¥ 12,800 | 8-10周 | ||
50 mg | ¥ 16,800 | 8-10周 | ||
100 mg | ¥ 21,500 | 8-10周 |
产品描述 | NHWD-870 is an effective and selective inhibitor of BET family bromodomain only binding to BRD2, BRD3, BRD4 (IC50 = 2.7 nM), and BRDT. NHWD-870 exhibits potent anti-tumor efficacies and suppresses cancer cell-macrophage interaction through the increase of tumor apoptosis and inhibition of tumor proliferation. |
靶点活性 | BRD4:2.7 nM |
体外活性 | NHWD-870 exhibits mild inhibition of the hERG channel (IC50 = 5.4 µM). NHWD-870 shows robust activities inducing apoptosis and suppressing cell proliferation. NHWD-870 (0.01-10000 nM) inhibits melanoma cells (A375) with an IC50 of 2.46 nM. In H526, A2780, ES-2, and MDA-MB231 cells, NHWD-870 (0-10000 nM; 5 days) suppressed cell growth. NHWD-870 (0-50 nM; 24 hours) inhibits BRD4 phosphorylation and c-MYC expression in H526, A2780, ES-2, and MDA-MB231 cells[1]. |
体内活性 | NHWD-870 (0.75-3 mg/kg; p.o.) reduces the number of tumor associated macrophages (TAMs) in subcutaneously implanted H526 and A2780 tumors. NHWD-870 downregulated CSF1 expression in tumor cells to inhibit TAM proliferation[1]. |
分子量 | 491.59 |
分子式 | C29H29N7O |
CAS No. | 2115742-03-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 60 mg/mL (122.05 mM), Sonication and heating to 60℃ are recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0342 mL | 10.1711 mL | 20.3422 mL | 50.8554 mL |
5 mM | 0.4068 mL | 2.0342 mL | 4.0684 mL | 10.1711 mL | |
10 mM | 0.2034 mL | 1.0171 mL | 2.0342 mL | 5.0855 mL | |
20 mM | 0.1017 mL | 0.5086 mL | 1.0171 mL | 2.5428 mL | |
50 mM | 0.0407 mL | 0.2034 mL | 0.4068 mL | 1.0171 mL | |
100 mM | 0.0203 mL | 0.1017 mL | 0.2034 mL | 0.5086 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
NHWD-870 2115742-03-3 Apoptosis Chromatin/Epigenetic Epigenetic Reader Domain NHWD870 melanoma cell-macrophage bromodomains Inhibitor inhibit oral selective NHWD 870 cancer interaction inhibitor