bgb-290

Name	(R)-2-fluoro-10a-methyl-7,8,9,10,10a,11-hexahydro-5,6,7a,11-tetraazacyclohepta[def]cyclopenta[a]fluoren-4(5H)-one
Synonyms	bgb-290 BGB 290 BGB290. BGB-290 EOS-61090 PAMIPARIB Pamiparib Pamiparib(BGB290) BGB-290,Pamiparib (R)-2-fluoro-10a-methyl-7,8,9,10,10a,11-hexahydro-5,6,7a,11-tetraazacyclohepta[def]cyclopenta[a]fluoren-4(5H)-one (R)-2-fluoro-10a-methyl-5,8,9,10,10a,11-hexahydro-5,6,7a,11-tetraazacyclohepta[def]cyclopenta[a]fluoren-4(7H)-one
CAS	1446261-44-4

Molecular Formula	C16H15FN4O
Molar Mass	298.31
Density	1.68±0.1 g/cm3(Predicted)
pKa	11.56±0.40(Predicted)
Storage Condition	Room Temprature
In vitro study	BGB-290 has effective DNA trapping activity, IC50 is 13 nM. In the cell experiment, BGB-290 can inhibit the formation of intracellular PAR, IC50 is 0.24 nM.
In vivo study	In a MDA-MB-436 breast cancer xenograft model with BRCA1 mutation, oral administration at BGB-290 resulted in time-and dose-dependent inhibition of PARylation, which correlated with intratumoral drug concentration. In a patient biopsy-derived model of small cell lung cancer, BGB-290 had potent activity in combination with other chemotherapies. In C57 mice, BGB-290 can significantly penetrate into the brain tissue. By the oral route, the ratio of the exposure in the brain and in the plasma BGB-290 is about 20%.