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Pamiparib

Chemical Structure : Pamiparib

CAS No.: 1446261-44-4

Pamiparib (BGB-290;BGB290)

Catalog No.: PC-60483Not For Human Use, Lab Use Only.

Pamiparib (BGB-290, BGB290) is a highly potent, selective and brain penetrant PARP1/2 inhibitor with IC50 of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively.

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Biological Activity

Pamiparib (BGB-290, BGB290) is a highly potent, selective and brain penetrant PARP1/2 inhibitor with IC50 of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively.
Pamiparib (BGB-290) is high selectivity over other PARP enzymes.
Pamiparib (BGB-290) shows potent DNA-trapping activity with IC50 of 13 nM in vitro.
Pamiparib (BGB-290) potently inhibits intracellular PAR formation with an IC50 of 0.24 nM in cellular assays,  is highly active both in vitro and in vivo in BRCA mutant tumor cells.
Oral administration of BGB-290 resulted in time-dependent and dose-dependent inhibition of PARylation in MDA-MB-436 (BRCA1 mutant) breast cancer xenograft, over 10-fold more potent than olaparib.

Physicochemical Properties

M.Wt 298.32
Formula C16H15FN4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(10aR)-2-fluoro-10a-methyl-5,8,9,10,10a,11-hexahydro-5,6,7a,11- tetraazacyclohepta[def]cyclopenta[a]fluoren-4(7H)-one

References

1. Zhiyu Tang, et al. Cancer Res (2015) 75 (15_Supplement): 1653.

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