CAY10749 is a dual inhibitor of poly(ADP-ribose) polymerase (PARP) and PI3K (IC50s = 6.03, 3.63, 5.62, and 7.41 nM for PARP1, PARP2, PI3Ka, and PI3KD, respectively).{50888} It is selective for these enzymes over PI3KB and PI3Ky (IC50s = 288.4 and 831.76 nM, respectively), as well as a panel of 374 additional kinases at 1 uM. CAY10749 (1 uM) induces dsDNA break formation in a neutral comet assay and apoptosis in MDA-MB-468 breast cancer cells. It inhibits proliferation of eight cancer cell lines, including pancreatic, ovarian, lymphoma, leukemia, and lung cancer cells, with IC50 values ranging from 398.11 to 2,818.38 nM. CAY10749 (50 mg/kg twice per day) reduces tumor growth by 73.4% in an MDA-MB-468 mouse xenograft model.
Specifications
Size
1 mg
CAS number
2337386-47-5
Supplier
Cayman Chemical
Shipping & storage
Shipping condition
Dry Ice
Storage temperature
-20°C