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BET bromodomain inhibitor 3

Cat. No. M41661
BET bromodomain inhibitor 3 Structure
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Biological Activity

BET bromodomain inhibitor 3 is BET bromodomain inhibitor.

Chemical Information
Molecular Weight 339.35
Formula C18H17N3O4
CAS Number 854137-39-6
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] King L Hung et al. Nature. ecDNA hubs drive cooperative intermolecular oncogene expression

[2] Michael Alexanian et al. Nature. A transcriptional switch governs fibroblast activation in heart disease

[3] Wenxin Du et al. Autophagy. The role of autophagy in targeted therapy for acute myeloid leukemia

[4] Hemant Kumar Bid et al. Oncoscience. BET bromodomain inhibitor (JQ1) and tumor angiogenesis

[5] Michael Zengerle et al. ACS Chem Biol. Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

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