Chemical Structure : BBI-2779
CAS No.:
2871057-47-3
BBI-2779
(BBI 2779)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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377.41
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Formula
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C19H19N7O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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5-((5-(2-((1R,2R)-2-aminocyclobutoxy)-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile
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References
1. Tang J, et al. Nature. 2024 Nov;635(8037):210-218.
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