BGT226

• CAT Number: I000973
• CAS Number: 1245537-68-1
• Molecular Formula: C₃₂H₂₉F₃N₆O₆
• Molecular Weight: 650.6
• Purity: ≥95%
• Target: PI3K
• Solubility: DMSO ≥125mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL
• Storage: 3 years -20C powder
• IC50: 4 nM/63 nM/38 nM(PI3Kα/β/γ) [1]
• InChI: InChI=1S/C28H25F3N6O2.C4H4O4/c1-35-24-16-33-22-6-3-17(18-4-8-25(39-2)34-15-18)13-20(22)26(24)37(27(35)38)19-5-7-23(21(14-19)28(29,30)31)36-11-9-32-10-12-36;5-3(6)1-2-4(7)8/h3-8,13-16,32H,9-12H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
• InChIKey: YUXMAKUNSXIEKN-BTJKTKAUSA-N
• SMILES: CN1C2=CN=C3C=CC(=CC3=C2N(C1=O)C4=CC(=C(C=C4)N5CCNCC5)C(F)(F)F)C6=CN=C(C=C6)OC.C(=CC(=O)O)C(=O)O

BGT226 (CAT: I000973) is a dual inhibitor of phosphoinositide 3-kinase (PI3K) and a mammalian target of rapamycin (mTOR). It effectively inhibits both PI3K and mTOR complexes, including PI3Kα, β, γ, δ, and mTORC1/2, with IC50 values ranging from 4 to 50 nM. BGT226 demonstrates potent antiproliferative activity against a variety of cancer cell lines and exhibits strong tumor growth inhibition in xenograft models. It induces cell cycle arrest and apoptosis by inhibiting downstream signaling pathways involved in cell survival and proliferation. BGT226 shows promise as a potential anticancer agent, targeting the PI3K/mTOR pathway, which is frequently dysregulated in various cancers.

Reference

[1]. Markman B, et al. Phase I safety, pharmacokinetic, and pharmacodynamic study of the oral phosphatidylinositol-3-kinase and mTOR inhibitor BGT226 in patients with advanced solid tumors. Ann Oncol, 2012, 23(9), 2399-2408.
[2]. Chang KY, et al. Novel phosphoinositide 3-kinase/mTOR dual inhibitor, NVP-BGT226, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo. Clin Cancer Res, 2011, 17(22), 7116-7126.
[3]. Baumann P, et al. Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma. Anticancer Drugs, 2012, 23(1), 131-138.