首页Cell Cycle/CheckpointCDKBI-9564
BI-9564
编号 T6786     别名: BI9564, BI 9564,
CAS 1883429-22-8     分子式 C20H23N3O3     分子量 353.42
靶点: BRD7; BRD9; CECR2;
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.
纯度:98.8%
规格 库存 单价 数量
2 mg 上海现货 489.00
5 mg 上海现货 679.00
10 mg 上海现货 1202.00
50 mg 上海现货 4907.00
100 mg 上海现货 7472.00
1 mL * 10 mM (in DMSO) 上海现货 679.00
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生物活性

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

BRD7,73nM(Kd)

BRD9,5.9nM(Kd)

CECR2,77nM(Kd)

体外活性

EOL-1, human acute myeloid eosinophilic leukemia cell line, was antiproliferative by BI-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)

细胞系: MV-4-11 cells

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.

动物模型:FeCIEA-NOG mice

化学信息

分子量

353.42

分子式

C20H23N3O3

CAS

1883429-22-8

溶解度

DMSO: 7.2 mg/mL, warmed

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 2.829 ml 14.147 ml 28.295 ml
5 mM 0.566 ml 2.829 ml 5.659 ml
10 mM 0.283 ml 1.415 ml 2.829 ml
50 mM 0.057 ml 0.283 ml 0.566 ml
相关化合物库
本产品收录于以下化合物库中:
  • 经典已知活性库
  • 抗癌化合物库
  • 表观遗传库
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