BI-7273 is a potent and selective BRD9 inhibitor with IC50s of 19 nM and 117 nM for BRD9 and BRD7, respectively. BI-7273 blocks EOL-1 cell proliferation with EC50 of 1400 nM. In vitro, BI-7273 (1 μM) is active in U2OS cell lines.
|Animal models||Female BomTac:NMRI-Foxn1nu mice|
|Dosages||20 and 180 mg/kg|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 40 mg/mL|
Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor.
Martin LJ, et al. J Med Chem. 2016 May 26;59(10):4462-75. PMID: 26914985.
|Related Epigenetic Reader Domain Products|
dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC50 of 14 nM.
dBET1 is a potent BRD4 protein degrader with an EC50 of 430 nM.
ABBV-744 is a BDII-selective BET bromodomain inhibitor that is used in the research of AML and metastic castration-resistant prostate cancer.
CPI-637 is a potent and selective CBP/EP300 bromodomains inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respectively.
GSK1324726A (I-BET726) is a highly selective inhibitor of BET family proteins with IC50 of 41 nM, 31 nM, and 22 nM for BRD2, BRD3, and BRD4, respectively.
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