Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Y06036 是一种选择性 BET 抑制剂,具有抗肿瘤活性,可与 BRD4(1)溴结构域结合,Kd 值为 82 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 258 | 现货 | ||
5 mg | ¥ 398 | 现货 | ||
10 mg | ¥ 663 | 现货 | ||
25 mg | ¥ 1,150 | 现货 | ||
50 mg | ¥ 1,830 | 现货 | ||
100 mg | ¥ 2,990 | 现货 | ||
500 mg | ¥ 6,730 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 455 | 现货 |
产品描述 | Y06036, a potent and selective BET inhibitor, can bind to the BRD4(1) bromodomain (Kd: 82 nM). |
靶点活性 | BRD4(1):82 nM (Kd, cell free) |
体外活性 | Y06036 bounds to the BRD4(1) bromodomain with Kd values of 82 nM. Y06036 potently inhibited cell growth, colony formation, and the expression of AR, AR-regulated genes, and MYC in prostate cancer cell lines. |
体内活性 | The mice were randomized and intraperitoneally (i.p.) treated with either vehicle or BET inhibitor Y06036 (50 mg/kg, 5 times per week) when the tumor volume reached approximately 100 mm3. Y06036 exhibited strong antitumor activities during the 25-day treatment period, with a tumor growth inhibition (TGI) of 70%. |
细胞实验 | LNCaP, C4-2B, 22Rv1, and VCaP prostate cancer cells were cultured in RPMI 1640 with 10% FBS at 37 °C and an atmosphere of 5% CO2. For cell viability, cells were seeded in 384-well plates at 500?1000 cells per well (optimum density for growth) in a total volume of 20 μL of media. After 12 h, 10 μL of chemical compounds with 2-fold or 3-fold serial dilution was added to each well with final concentration from 5 nM to 100 μM. The measurement was conducted 96 h after seeded for LNCaP, C4-2B, and 22Rv1 and 144 h after seeded for VCaP. Then, 25 μL of CellTiter-GLO reagents was added, and luminescence was measured on GLOMAX microplate luminometer, according to the manufacturer's instructions. The estimated in vitro half-maximal inhibitory concentration (IC50) values were calculated using Prism 6 software. |
动物实验 | Four-week-old male mice (strain: C.B-17/IcrHsd-Prkdcscid for C4-2B) were used for tumor inoculation. Each mouse was inoculated subcutaneously at the dorsal flank on both sides of the mice with C4-2B tumor cells (2 × 10^6 cells) in a mixture of 100 μL PBS and Matrigel (1:1). When the tumor volume reached approximately 100 mm3, the mice were randomized into groups (n = 5?7 per group) and then treated intraperitoneally (ip) with 100 μL of either vehicle or Y06036 and 7m (in a formulation of 15% Cremophor EL, Calbiochem, 82.5% PBS, and 2.5% DMSO) five times per week. The length (L) and width (W) of the tumor mass were monitored by calipers, and volume was expressed in mm3 calculated with the equation V = (π/6)(L × W2). Tumor growth inhibition (TGI) was calculated using the equation TGI = [1 ? (T ? T0)/(C ? C0)] × 100, wherein T and T0 are the mean tumor volumes on a specific experimental day and on the first day of treatment, respectively, for the test groups; and likewise C and C0 are the mean tumor volumes for the vehicle group. |
分子量 | 427.27 |
分子式 | C16H15BrN2O5S |
CAS No. | 1832671-96-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (234 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3404 mL | 11.7022 mL | 23.4044 mL | 58.511 mL |
5 mM | 0.4681 mL | 2.3404 mL | 4.6809 mL | 11.7022 mL | |
10 mM | 0.234 mL | 1.1702 mL | 2.3404 mL | 5.8511 mL | |
20 mM | 0.117 mL | 0.5851 mL | 1.1702 mL | 2.9256 mL | |
50 mM | 0.0468 mL | 0.234 mL | 0.4681 mL | 1.1702 mL | |
100 mM | 0.0234 mL | 0.117 mL | 0.234 mL | 0.5851 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。
Y06036 1832671-96-1 Chromatin/Epigenetic Epigenetic Reader Domain inhibit Inhibitor Y 06036 Y-06036 inhibitor