BBT-176 | EGFR C797S inhibitor | Probechem Biochemicals

Chemical Structure : BBT-176

BBT-176 (BBT176)

Catalog No.: PC-23647Not For Human Use, Lab Use Only.

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Biological Activity

BBT-176 is a potent, mutant-selective fourth-generation inhibitor of EGFR C797S mutations with IC50 of 4.36, 1.79, and 5.35 nM for EGFR 19Del/C797S, EGFR 19Del/T790M/C797S, and EGFR L858R/C797S, respectively.
BBT-176 selectively and noncovalently inhibits triple-mutant EGFR 19Del/T790M/C797S and L858R/T790M/C797S at nanomolar concentrations.
BBT-176 has IC50 of 42, 49, 183, and 202 nM against Ba/F3 cells expressing EGFR 19Del/C797S, EGFR 19Del/T790M/C797S, EGFR L858R/C797S, and EGFR L858R/T790M/C797S, respectively.
BBT-176 strongly inhibited the tumor growth, and in some conditions induced tumor regression in mouse models.

Physicochemical Properties

M.Wt	587.14
Formula	C27H35ClN8O3S
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	N-(2-((5-chloro-2-((2-methoxy-4-(4-(piperazin-1-yl)piperidin-1-yl)phenyl)amino)pyrimidin-4-yl)amino)phenyl)methanesulfonamide

References

1. Lim SM, et al. Clin Cancer Res. 2023 Aug 15;29(16):3004-3016.

BBT-176 (BBT176)

Biological Activity

Physicochemical Properties

References

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