Formulation: A solid
Formal Name: N-[(8S)-4-amino-8,9-dihydro-6-methyl-5-(3-quinolinyl)pyrimido[5,4-b]indolizin-8-yl]-2-propenamide
Purity: ≥98%
Formula Markup: C23H20N6O
Formula Weight: 396,4
Shelf life (days): 1460
CAS Number: 1661854-97-2
Notes: TAS 6417 is a pan-EGFR inhibitor.{49831} It inhibits wild-type EGFR (IC50= 8 nM), as well as the EGFR point mutants EGFRL858R, EGFRL861Q, EGFRT790M, EGFRT790M/L858R (IC50s = 1.9, 5.5, 4.1, and 2 nM, respectively) and the insertion or deletion mutants EGFR D770_N771insNPG, EGFR d746-750, and EGFR d746-770/T790M (IC50s = 7.4, 1.4, and 1.1 nM, respectively). It is selective for these kinases over a panel of 20 additional kinases (IC50s = 44-850 nM) but does inhibit TXK, BMX, HER4, Tec, and BTK (IC50s = 1.1-22 nM). TAS 6417 inhibits the proliferation of LXF 2478L, H1975, HCC827, and PC-9 lung cancer cells (GI50s = 86.5, 45.4, 1.92, and 2.96 nM, respectively). In vivo, TAS 6417 (50, 100, and 200 mg/kg) reduces tumor volume and increases survival in an H1975 EGFR D770-N771insSVD mouse xenograft model.
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