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PROTAC BRD4 Degrader-20

Cat. No. M41653
PROTAC BRD4 Degrader-20 Structure
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Biological Activity

PROTAC BRD4 Degrader-20 is an bifunctional compound and an degrader of BRD4.

Chemical Information
Molecular Weight 1056.69
Formula C55H58ClN9O7S2
CAS Number 2086300-61-8
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] Yi Shi et al. Cell Discov. BRD4-targeting PROTAC as a unique tool to study biomolecular condensates

[2] Martin P Schwalm et al. Curr Opin Chem Biol. BET bromodomain inhibitors

[3] Zhenyi Hu et al. Chembiochem. Recent Developments in PROTAC-Mediated Protein Degradation: From Bench to Clinic

[4] Marı A Maneiro et al. ACS Chem Biol. Antibody-PROTAC Conjugates Enable HER2-Dependent Targeted Protein Degradation of BRD4

[5] Morgan S Gadd et al. Nat Chem Biol. Structural basis of PROTAC cooperative recognition for selective protein degradation

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  Catalog
Abmole Inhibitor Catalog




Keywords: PROTAC BRD4 Degrader-20 supplier, Epigenetic Reader Domain, inhibitors, activators


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