BI 894999 ( BI894999 )

Catalog No. M12534 CAS No. 1660117-38-3

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

BI 894999
Note

Research use only, not for human use.
Brief Description

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

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
Synonyms

BI894999
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

Bromodomain
Research Area

Cancer
Indication

Solid Tumors

CAS Number

1660117-38-3
Formula Weight

429.52
Molecular Formula

C25H27N5O2
Purity

>98% (HPLC)
Solubility

——
SMILES

CN1C(C(C)=CC(C2=NC3=CN=C(C4CCOCC4)C=C3N2[C@@H](C)C5=CC=CC=C5)=N1)=O
Chemical Name

(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.

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