Formulation: A solid
Formal Name: N-[(1R)-1-[3-amino-5-(trifluoromethyl)phenyl]ethyl]-7-methoxy-2-methyl-6-[[(3S)-tetrahydro-3-furanyl]oxy]-4-quinazolinamine
Purity: ≥98%
Formula Markup: C23H25F3N4O3
Formula Weight: 462,5
Shelf life (days): 1460
CAS Number: 2230836-55-0
Notes: BI-3406 is an inhibitor of the protein-protein interaction between K-Ras and the guanine nucleotide exchange factor son of sevenless homolog 1 (SOS1; IC50 = 5 nM).{62502} It selectively disrupts the protein-protein interaction between K-RasG12C or K-RasG12D with SOS1 over SOS2, and it is selective over 321 kinases in a panel at 10 µM but does inhibit PLK4, BMPR2, and LRRK2 activity by greater than 50%. BI-3406 inhibits the growth of DLD-1, A549, NCI H23, and NCI H358 cells expressing mutant K-Ras (IC50s = 16-52 nM) but not NCI H520 and A375 cells expressing wild-type K-Ras. BI-3406 (12 or 50 mg/kg, twice per day) reduces tumor growth in an MIA PaCa-2 mouse xenograft model.
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