Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BRD9500 是一种具有口服活性的磷酸二酯酶 3 (PDE3) 抑制剂,对PDE3A 和PDE3B 的IC50分别为 10 和 27 nM。BRD9500 在黑色素瘤细胞系 SK-MEL-3 癌症异种移植模型中具有活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 2,390 | 5日内发货 | ||
10 mg | ¥ 3,990 | 5日内发货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,650 | 5日内发货 |
产品描述 | BRD9500 is an orally active inhibitor of phosphodiesterases 3 (PDE3) with IC 50 s of 10 and 27 nM for PDE3A and PDE3B, respectively. BRD9500 is active in an SK-MEL-3 xenograft model of cancer [1]. |
体外活性 | BRD9500 is a DNMDP analog. DNMDP potently and selectively inhibits PDE3A and PDE3B and kills cancer cells by inducing PDE3A/B interactions with SFLN12 [1]. BRD9500 exhibits an EC 50 of 1 nM for SK-MEL-3 melanoma cell line viability [1]. BRD9500 exhibits an EC 50 of 1.6 nM for HeLa viability [1]. BRD9500 (10 μM; 8 hours) stabilizes the PDE3A-SLFN12 interaction in HeLa cells [1]. Western Blot Analysis [1] Cell Line: HeLa cells Concentration: 10 μM Incubation Time: 8 hours Result: SLFN12 coimmunoprecipitation was analyzed by immunoblotting with an anti-V5 antibody to detect the SLFN12-V5 fusion protein. The SLFN12-V5 was clearly detected with the anti-V5 antibody. |
体内活性 | BRD9500 (10, 20, and 50 mg/kg; orally) inhibits SK-MEL-3 melanoma growth in mice [1]. BRD9500 shows high plasma levels in mice after iv (1 mg/kg) as well as po (2 mg/kg) dosing over eight hours making it a valuable candidate for in vivo xenograft testing [1]. Animal Model: Female NMRI nude mice bearing SK-MEL-3 melanoma cells tumor xenografts [1] Dosage: 10, 20, and 50 mg/kg Administration: Orally at 10 and 20 mg/kg twice daily (2QD) and at 50 mg/kg once per day (QD). Result: Achieved the strongest antitumor activity at 50 mg/kg. All treatments were well tolerated without critical body weight loss or toxicities. |
分子量 | 291.32 |
分子式 | C15H18FN3O2 |
CAS No. | 1630760-75-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
BRD9500 1630760-75-6 Inhibitor inhibitor inhibit