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BI-9564 — Datasheet

CAT. NO. DC9888

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ParameterValue
Chemical Name4-[4-[(Dimethylamino)methyl]-2,5-Dimethoxy-Phenyl]-2-Methyl-2,7-Naphthyridin-1-One
CAS No.1883429-22-8
SynonymsBI-9564;BI 9564;4-(4-Dimethylaminomethyl-2,5-dimethoxy-phenyl)-2-methyl-2H-[2,7]naphthyridin-1-one;4-[4-[(Dimethylamino)methyl]-2,5-dimethoxyphenyl]-2-methyl-2,7-naphthyridin-1-one;GTPL8950;4-(4-((dimethylamino)methyl)-2,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one;4-[4-[(Dimethylamino)methyl]-2,5-Dimethoxy-Phenyl]-2-Methyl-2,7-Naphthyridin-1-One;4-[4-[(Dimethylamino)methyl]-2,5-dimethoxyphenyl]-2-methyl-1,2-dihydro-2,7-naphthyridin-1-one;4-{4-[(dimethylamino)methyl]-2,5-dimethoxyphenyl}-2-methyl-1,2-dihydro-2,7-naphthyridin-1-one;5U6;BCP17135;BDBM50183449;BI9564;s8113
FormulaC20H23N3O3
M.Wt353.4149
SMILESO(C([H])([H])[H])C1C([H])=C(C(=C([H])C=1C1=C([H])N(C([H])([H])[H])C(C2C([H])=NC([H])=C([H])C1=2)=O)OC([H])([H])[H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H]
Purity>98%

Biological Activity

BI-9564 is a selective, and cell-permeable BRD9 BD inhibitor, with Kd of 5.9 nM for BRD9, and IC50 of > 100 μM for BET family.

In Vitro

BI-9564 (<5 μM) shows no activity against 324 kinases, and at 10 μM, an inhibition >40% is observed for only 2 out of 55 GPCRs. BI-9564 has antiproliferative effect on human acute myeloid eosinophilic leukemia cell line EOL-1, with EC50 of 800 nM[1]. BI-9564 shows Kd of 73 nM for BRD7, and is >10-fold more selective for BRD9 over the highly homologues bromodomain BRD7, which has been implied as a tumor suppressor and is down-regulated in cancer cells[2].

In Vivo

BI-9564 (180 mg/kg, p.o.) shows attractive ADME/PK profiles for in vivo proof-of-concept studies. BI-9564 results in a modest but significant additional survival benefit of 2 days compared to survival of the control group in a xenograft model of human AML[1].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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