Shelf life (days): 1460.0
Formulation: A solid
Formal Name: N-[2-chloro-5-[4-[[(1R)-1-phenylethyl]amino]-6-quinazolinyl]-3-pyridinyl]-methanesulfonamide
Purity: ≥98%
Formula Markup: C22H20ClN5O2S
Formula Weight: 453.945
CAS Number: 2791417-66-6
Notes: An EGFR antagonist and PI3K inhibitor; selectively inhibits EGFR over HER2 and HER4 (IC50s = 14.7, 2,500, and >10,000 nM, respectively) and PI3Kδ, PI3Kα, and PI3Kγ over PI3Kβ (IC50s = 1.1, 6.4, 8.3, and 233 nM, respectively) but also inhibits DNA-PK (IC50s = 5.4 nM); induces gene expression in a reporter assay using HEK293 cells expressing PPARγ (EC50 = 3.4 µM); decreases phosphorylated levels of Akt and 4E-BP1 and induces apoptosis in CAL-33 tongue squamous cell carcinoma cells at 3 to 10 µM; reduces tumor volume and increases survival in a CAL-33 mouse xenograft model at 100 mg/kg per day
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