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BI-8128

Chemical Structure : BI-8128

CAS No.: 2769714-36-3

BI-8128 (BI 8128)

Catalog No.: PC-21465Not For Human Use, Lab Use Only.

BI-8128 is a potent, selective, reversible and orally bioavailable fourth generation EGFR inhibitor, potently inhibits oncogenic EGFR variants del19 and L858R as well as the acquired EGFR resistance mutations T790M and C797S.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

BI-8128 is a potent, selective, reversible and orally bioavailable fourth generation EGFR inhibitor, potently inhibits oncogenic EGFR variants del19 and L858R as well as the acquired EGFR resistance mutations T790M and C797S.
BI-8128 demonstrates potent, low nanomolar anti-proliferative activity in Ba/F3 cells that are dependent on the activity of human EGFR variants del19, del19 T790M C797S, L858R, and L858R T790M C797S.
BI-8128 potently inhibits the two major primary oncogenic EGFR variants del19 and L858R, in the presence and absence of the acquired EGFR resistance mutations T790M and C797S, while sparing wild-type EGFR.

Physicochemical Properties

M.Wt 610.72
Formula C32H38N10O3
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

(1R,4R)-5-(2-(4-(2-methoxyethyl)piperazin-1-yl)-6-(6-(4-methoxypyridin-3-yl)-4-methyl-1H-pyrazolo[4,3-c]pyridin-1-yl)-1-methyl-1H-imidazo[4,5-c]pyridin-4-yl)-2-oxa-5-azabicyclo[2.2.1]heptane

References

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