Description
A dual inhibitor of PARP and PI3K (IC50s = 6.03, 3.63, 5.62, and 7.41 nM for PARP1, PARP2, PI3Kα, and PI3Kδ, respectively); selective for these enzymes over PI3Kβ and PI3Kγ (IC50s = 288.4 and 831.76 nM, respectively) and a panel of 374 additional kinases at 1 µM; induces dsDNA break formation in a neutral comet assay and apoptosis in MDA-MB-468 breast cancer cells at 1 µM; inhibits proliferation of eight cancer cell lines (IC50s = 398.11-2,818.38 nM); reduces tumor growth by 73.4% in an MDA-MB-468 mouse xenograft model at 50 mg/kg twice per day ,,
Formal name: 4-[[3-[[2-[6-amino-4-(trifluoromethyl)-3-pyridinyl]-5,8-dihydro-4-(4-morpholinyl)pyrido[3,4-d]pyrimidin-7(6H)-yl]carbonyl]-4-fluorophenyl]methyl]-1(2H)-phthalazinone
Synonyms:
Molecular weight: 660.6
CAS: 2337386-47-5
Purity: ≥98%
Formulation: A crystalline solid
