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. Pamiparib shows potent DNA-trapping activity with an IC50 of 13 nM. Pamiparib inhibits intracellular PAR formation with an IC50 of 0.24 nM.
In vivo, oral administration of BGB-290 results in time-dependent and dose-dependent inhibition of PARylation in MDA-MB-436 (BRCA1 mutant) breast cancer xenograft. BGB-290 has significant brain penetration in C57 mice. The drug exposure in brain vs. that in plasma was close to 20% after oral administration of BGB-290.
|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.
|Solubility||DMSO ≥ 30 mg/mL|
BGB-290: A highly potent and specific PARP1/2 inhibitor potentiates anti-tumor activity of chemotherapeutics in patient biopsy derived SCLC models.
Zhiyu Tang, et al. Cancer Research. 2015 Aug;Volume 75, Issue 15.
Inhibition of PARP activity by BGB-290 potentiates efficacy of NSC 362856 in patient derived xenografts of glioblastoma multiforme.
Shiv K. Gupta, et al. Cancer Research. 2015 Aug;Volume 75, Issue 15.
|Related PARP Products|
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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.
RBN-2397 is a potent and orally active NAD+ competitive inhibitor of PARP7 (IC50<3 nM).
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