Chemical Structure : BBI-2779
货号: PC-23369Not For Human Use, Lab Use Only.
BBI-2779 is a potent, selective and orally bioavailable inhibitor of CHK1 with biochemical IC50 of 0.5 nM and cellular IC50 of 3 nM (pCHK1-S345 activity in HT29 cells), 160-fold selective for CHK1 over CHK2.
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BBI-2779 is a potent, selective and orally bioavailable inhibitor of CHK1 with biochemical IC50 of 0.5 nM and cellular IC50 of 3 nM (pCHK1-S345 activity in HT29 cells), 160-fold selective for CHK1 over CHK2.
BBI-2779 has superior biochemical and selective cell growth inhibition compared to other orally bioavailable CHK1 inhibitors.
BBI-2779 preferentially kills ecDNA-containing tumour cells, exhibits antiproliferation activity in COLO320DM cells with IC50 of 6 nM.
BBI-2779 suppresses tumour growth and prevents ecDNA-mediated acquired resistance to the pan-FGFR inhibitor infigratinib in gastric cancer model containing FGFR2 amplified on ecDNA, resulting in potent and sustained tumour regression in mice.
分子量 | 377.41 | |
分子式 | C19H19N7O2 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Tang J, et al. Nature. 2024 Nov;635(8037):210-218.
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