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BI 894999

Cat. No. M20727
BI 894999 Structure
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Biological Activity

BI 894999 is a potent and selective BET inhibitor with IC50 of 5 nM and 41 nM for the binding of BRD4-BD1 and BRD4-BD2 to acetylated histones, respectively. BI 894999 is highly selective for BRD2/3/4 and BRDT (Kd of 0.49-1.6 nM), with at least a 200-fold selectivity vs. BRD4-BD1.

Chemical Information
Molecular Weight 429.51
Formula C25H27N5O2
CAS Number 1660117-38-3
Solubility (25°C) DMSO 86 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Ulrike Tontsch-Grunt, et al. Br J Cancer. Therapeutic impact of BET inhibitor BI 894999 treatment: backtranslation from the clinic

[2] Daniel Gerlach, et al. Oncogene. The novel BET bromodomain inhibitor BI 894999 represses super-enhancer-associated transcription and synergizes with CDK9 inhibition in AML

[3] Ulrike Tontsch-Grunt, et al. Cancer Lett. Synergistic activity of BET inhibitor BI 894999 with PLK inhibitor volasertib in AML in vitro and in vivo

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