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BBI-2779

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

M.Wt 377.41
Formula C19H19N7O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-((5-(2-((1R,2R)-2-aminocyclobutoxy)-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile

References

1. Tang J, et al. Nature. 2024 Nov;635(8037):210-218.

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