| Identification | Back Directory | [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 | [CAS]
1446261-44-4 | [Synonyms]
bgb-290
EOS-61090
Pamiparib
Pamiparib(BGB290)
BGB-290,Pamiparib
PAMIPARIB; BGB-290; BGB 290; BGB290.
(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
5,6,7a,11-Tetraazacyclohepta[def]cyclopenta[a]fluoren-4(7H)-one, 2-fluoro-5,8,9,10,10a,11-hexahydro-10a-methyl-, (10aR)- | [Molecular Formula]
C16H15FN4O | [MDL Number]
MFCD30489383 | [MOL File]
1446261-44-4.mol | [Molecular Weight]
298.31 |
| Chemical Properties | Back Directory | [density ]
1.68±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF:20.0(Max Conc. mg/mL);67.04(Max Conc. mM)
DMF:PBS (pH 7.2) (1:10):0.09(Max Conc. mg/mL);0.3(Max Conc. mM)
DMSO:40.83(Max Conc. mg/mL);136.88(Max Conc. mM)
Ethanol:45.0(Max Conc. mg/mL);150.84(Max Conc. mM) | [form ]
A solid | [pka]
11.56±0.40(Predicted) |
| Hazard Information | Back Directory | [Description]
Pamiparib (BGB-290) is an investigational small molecule inhibitor of PARP1 and PARP2. Pamiparib is being evaluated as a monotherapy in pivotal clinical trials in China in recurrent platinum-sensitive and BRCA1/2 mutated ovarian cancers. | [Uses]
Pamiparib, is a PARP inhibitor, which can be used as an anticancer agent. | [in vivo]
Oral administration of Pamiparib results in time-dependent and dose-dependent inhibition of PARylation in MDA-MB-436 (BRCA1 mutant) breast cancer xenograft, correlating well with the tumor drug concentrations. It has also demonstrated good combination activity with chemotherapeutics in patient biopsy derived SCLC models. Also Pamiparib 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. | [storage]
Store at -20°C |
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