Usp1-in-1 (Formula I), an allosteric INHIBITOR of USP1, has been used IN cancer studies alone or IN combination with PARP inhibition.
|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 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.
|Related PARP Products|
GeA-69 is a cell-penetrating selective allosteric inhibitor targeting Macrodomain 2 (MD2) with a Kd of 2.1 µM.
RBN012759 is a potent, selective and orally active PARP14 inhibitor with IC50 values of <3 nM and 5 nM against the human and mouse catalytic domains, respectively. AIDS in the anti-tumor immune response.
Fluzoparib (SHR3162) is an effective oral active PARP1 inhibitor (IC50=1.46±0.72 nM) with superior antitumor activity. Fluzoparib selectively inhibited the proliferation of homologous recombination repair (HR) deficient cells and sensitized HR deficient cells to cytotoxic drugs. Fluzoparib has good pharmacokinetic properties in vivo and can be used in cancer research.
AZD5305 is a potent and oral active, second-generation PARP (highly selective PARP1) inhibitor.
BRCA1-IN-2 is a cell-permeable protein-protein interaction (PPI) inhibitor for BRCA1, with IC50 of 0.31 μM and Kd of 0.3 μM.
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