Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BI-9564 是一种选择性的且可透过细胞的 BRD9/BRD7溴结构域抑制剂,IC50分别为 75 和 3.4 μM,Kd 为 14 和 239 nM。它对 BET 家族的 IC50值大于 100 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 218 | 现货 | ||
5 mg | ¥ 497 | 现货 | ||
10 mg | ¥ 913 | 现货 | ||
25 mg | ¥ 1,980 | 现货 | ||
50 mg | ¥ 3,580 | 现货 | ||
100 mg | ¥ 5,230 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 547 | 现货 |
产品描述 | BI-9564, a specific cell-permeable BRD9 BD inhibitor. The Kd for BRD9 is 5.9 nM, and IC50 for BET family is > 100 μM. |
靶点活性 | BRD9:Kd: 20 nM |
体外活性 | EOL-1, human acute myeloid eosinophilic leukemia cell line, was antiproliferative byBI-9564 with EC50 of 800 nM.BRD7 implied as a tumor suppressor and is down-regulated in cancer cells, BI-9564 shows Kd of 73 nM for it, and is >10-fold more selective for BRD9 over the high homologues bromodomain. BI-9564 (<5 μM) shows no activity against 324 kinases, when BI-9564 at 10 μM, an inhibition >40% is observed for only 2 out of 55 GPCRs. |
体内活性 | In vivo proof-of-concept studies, BI-9564 (180 mg/kg, p.o.) shows attractive ADME/PK profiles. Compared to survival of the control group in a xenograft model of human AML, BI-9564 results in a modest but significant additional survival benefit of 2 days. |
细胞实验 | To 750,000 MV-4-11 cells in 250 μl growth medium (in IMDM, 10 % FBS, GlutaMAX, 25 mM HEPES and 0,1% 2-Mercaptoethanol) per well compound is added at the desired concentration from a 10 mM stock solution using the HP D300 Digital Dispenser. After 2 hours of incubation with the compound, cells are collected by centrifugation, washed in ice cold PBS and lysed in 15 μl of cell extraction buffer. After 30 minutes on ice, nucleic acids are disrupted by sonication. cMYC levels are measured using the human c-Myc (Total) ELISA Kit. (Only for Reference) |
动物实验 | Female CIEA-NOG mice engrafted intravenously with 1×107 EOL-1 AML cells, which express stably luciferase and GFP, were administered orally on day 5 with BI-9564(10 mL/kg body weight), which is formulated with 0.5% Natrosol. |
别名 | BI 9564, BI9564 |
分子量 | 353.41 |
分子式 | C20H23N3O3 |
CAS No. | 1883429-22-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 3.53 mg/mL (10 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.8296 mL | 14.1479 mL | 28.2957 mL | 70.7394 mL |
5 mM | 0.5659 mL | 2.8296 mL | 5.6591 mL | 14.1479 mL | |
10 mM | 0.283 mL | 1.4148 mL | 2.8296 mL | 7.0739 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。
BI-9564 1883429-22-8 Chromatin/Epigenetic Epigenetic Reader Domain BI 9564 BI9564 Inhibitor inhibit inhibitor