BI 894999 (Amredobresib) | BRD4 inhibitor | Probechem Biochemicals

Chemical Structure : BI 894999

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BI 894999 (Amredobresib, BI-894999)

货号: PC-38620Not For Human Use, Lab Use Only.

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

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生物&药学活性

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

物理化学性质&存储条件

分子量	467.581
分子式	C26H29N9
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	6-(1-benzyl-6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)-N,3-dimethyl-[1,2,4]triazolo[4,3-a]pyrazin-8-amine

参考文献

1. Tontsch-Grunt U, et al. Cancer Lett. 2018 May 1;421:112-120.

2. Gerlach D, et al. Oncogene. 2018 May;37(20):2687-2701.

BI 894999 (Amredobresib, BI-894999)

生物&药学活性

物理化学性质&存储条件

参考文献

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BI 894999 (Amredobresib, BI-894999)

生物&药学活性

物理化学性质&存储条件

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