BI 894999 ( BI894999 )

产品货号. M12534 CAS No. 1660117-38-3

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

拼团产品询价大包装询价加入购物车

产品名称

BI 894999
注意事项

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
产品简述

BI 894999 is a novel potent, selective BET inhibitor with IC50 of 5 and 41 nM for BRD4-BD1 and BRD4-BD2 bromodomains, respectively.
产品描述

BI 894999 is a novel potent, selective BET inhibitor with IC50 of 5 and 41 nM for BRD4-BD1 and BRD4-BD2 bromodomains, respectively; displays excellent selectivity over other bromodomains; decreases S-Phase and increases apoptosis, Volasertib augments and prolongs the decrease of MYC expression caused by BI 894999 treatment in AML cell lines; dramatically reduces tumor burden accompanied by eradication of AML cells in mouse bone marrow combined with Volasertib; also represses super-enhancer-associated transcription and synergizes with CDK9 inhibition in AML.Solid Tumors Phase 1 Clinical
同义词

BI894999
通路

Chromatin/Epigenetic
靶点

Bromodomain
受体

Bromodomain
研究领域

Cancer
适应症

Solid Tumors

CAS Number

1660117-38-3
分子量

429.52
分子式

C25H27N5O2
纯度

>98% (HPLC)
溶解度

——
SMILES

CN1C(C(C)=CC(C2=NC3=CN=C(C4CCOCC4)C=C3N2[C@@H](C)C5=CC=CC=C5)=N1)=O
化学全称

(S)-2,4-dimethyl-6-(1-(1-phenylethyl)-6-(tetrahydro-2H-pyran-4-yl)-1H-imidazo[4,5-c]pyridin-2-yl)pyridazin-3(2H)-one

1. Tontsch-Grunt U, et al. Cancer Lett. 2018 Feb 14;421:112-120.
2. Gerlach D, et al. Oncogene. 2018 Mar 1. doi: 10.1038/s41388-018-0150-2.

计算器

产品手册

关联产品

BRD4 inhibitor Compo...

BRD4 inhibitor Compound V is a domain-selective inhibitor of BRD4 with IC50 of 1.8 uM for BRD4 BD1, displays 6- and 16-fold selectivity for BRD4 over BRD2 and BRD3, respectively.
GNE-371

GNE-371 (GNE371) is a highly potent and selective chemical probe for the second bromodomain of TAF1 (TAF1(2)) with IC50/Kd of 10/1 nM.
BI 894999

BI 894999 is a novel potent, selective BET inhibitor with IC50 of 5 and 41 nM for BRD4-BD1 and BRD4-BD2 bromodomains, respectively.