BI-7273

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效、选择性和细胞渗透性的 BRD9 bromodomain 抑制剂，在 Alpha 测定中 IC50 为 19 nM。

A potent, selective and cell-permeable BRD9 bromodomain inhibitor with IC50 of 19 nM in Alpha assay; displays >5-fold selectiveity over BRD7, and >5,000-fold over BRD4-BD1, BRD4-BD2, and BRD2-BD1; blocks EOL-1 cell proliferation with EC50 of 1.4 uM, and displays antitumor activity in an AML xenograft model.

BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM. BI-7273 also has slight activity against a panel of kinases such as CECR2, BRPF1, BRD1, CREBBP, EP300, FALZ, TAF1(2) and TAF1L(2), with Kds of 8.8 nM, 210 nM, 2600 nM, 8600 nM, 10000 nM, 850 nM, 1000 nM, and 1200 nM, respectively. BI-7273 (1 μM) is active in U2OS cell lines. BI-7273 blocks EOL-1 cell proliferation with EC50 of 1400 nM.

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BI7273 | BI 7273

Chromatin/Epigenetic

Bromodomain

BRD7|BRD9

Cancer

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1883429-21-7

353.4149

C20H23N3O3

>98% (HPLC)

DMSO: 10 mg/mL

O=C1N(C)C=C(C2=CC(OC)=C(CN(C)C)C(OC)=C2)C3=CC=NC=C13

2,7-Naphthyridin-1(2H)-one, 4-[4-[(dimethylamino)methyl]-3,5-dimethoxyphenyl]-2-methyl-

(-20℃)

With Ice Pack

≥ 2 years