PI3K/mTOR Inhibitor-4

• CAT Number: I042766
• CAS Number: 2361215-32-7
• Molecular Formula: C27H22FN3O6S
• Molecular Weight: 535.54
• Purity: ≥95%
• Synonyms: 4-fluoro-N-[2-methoxy-5-[4-(4-methoxyphenyl)-3-oxo-1,4-benzoxazin-6-yl]pyridin-3-yl]benzenesulfonamide
• InChI: InChI=1S/C27H22FN3O6S/c1-35-21-8-6-20(7-9-21)31-24-14-17(3-12-25(24)37-16-26(31)32)18-13-23(27(36-2)29-15-18)30-38(33,34)22-10-4-19(28)5-11-22/h3-15,30H,16H2,1-2H3
• InChIKey: MVOGBVAVCQDEHO-UHFFFAOYSA-N
• SMILES: COC1=CC=C(C=C1)N2C(=O)COC3=C2C=C(C=C3)C4=CC(=C(N=C4)OC)NS(=O)(=O)C5=CC=C(C=C5)F

PI3K/mTOR Inhibitor-4 is an orally active pan-class I PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-4 has enzymatic inhibition activity for PI3Kα, PI3Kγ, PI3Kδ and mTOR with IC50 values of 0.63 nM, 22 nM, 9.2 nM and 13.85 nM, respectively. PI3K/mTOR Inhibitor-4 can be used for the research of cancer[1].
PI3K/mTOR Inhibitor-4 (compound 8d-1) has enzymatic inhibition activity for PI3Kα, PI3Kδ, mTOR, PI3Kβ and PI3Kγ with IC50 values of 0.63 nM, 9.2 nM, 13.85 nM, 94.54 nM and 22 nM, respectively[1].
PI3K/mTOR Inhibitor-4 shows potent anti-proliferation activity in A549, Hela, HCT-116, HepG2, A375 and MCF-7 cells with IC50 values of 1.35 nM, 1.22 nM, 13.44 nM, 1.08 nM, 18.4 nM and 8.26 nM, respectively[1].
PI3K/mTOR Inhibitor-4 (2.5-10 µM; 24 h) inhibits the PI3K/AKT/mTOR pathway[1].
PI3K/mTOR Inhibitor-4 (compound 8d-1) (i.v., oral; 1mg/kg, 10 mg/kg) displays favorable pharmacokinetic parameters in Sprague−Dawley rats[1].
PI3K/mTOR Inhibitor-4 (oral; 10-50 mg/kg) shows significant efficiency in Hela/A549 tumor xenograft models without causing significant weight loss and toxicity[1].

Reference

[1]. Guoyi Yan, et al. Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. Eur J Med Chem
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