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QCA570

Cat. No. M10877
QCA570  Structure
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Biological Activity

QCA570 is made up of Cereblon ligands and BET ligands connected to PROTAC, which is paired with the BRD4 BD1 protein IC50 The value is 10 nM.

Chemical Information
Molecular Weight 695.79
Formula C39H33N7O4S
CAS Number 2207569-08-0
Solubility (25°C) DMSO ≥ 20 mg/mL
Storage -20°C,protect from light,dry,sealed
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] Chong Qin, et al. J Med Chem. Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression

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