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BI-9564
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BI-9564图片
CAS NO:1883429-22-8
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
BI9564
BI 9564
产品介绍
BI9564 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。
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.

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.

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.

Cas No.

1883429-22-8

分子式

C20H23N3O3

分子量

353.422

别名

BI9564;BI 9564

储存和溶解度

DMSO:10mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years