RBN-2397 is a potent and orally active NAD+ competitive inhibitor of PARP7 (IC50<3 nM). RBN-2397 selectively binds to PARP7 (Kd=0.001 μM) and restores interferon (Type I) signaling. RBN-2397 (0.0001-100 μM; 24 hours) inhibits cells proliferation with an IC50 value of 20 nM in NCI-H1373 lung cancer cells.
RBN-2397 (3-100 mg/kg; oral; once daily) 24-32 days treatment induces tumor-specific adaptive immune memory in CT26 syngeneic model with durable complete responses in CT26 tumor-bearing BALB/c mice.
|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|
Usp1-in-1 (Formula I), an allosteric INHIBITOR of USP1, has been used IN cancer studies alone or IN combination with PARP inhibition.
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.
Pamiparib (BGB-290) is an orally active, potent, highly selective inhibitor of PARP1 and PARP2 with IC50 values of 0.9 nM and 0.5 nM, respectively.
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