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1、BGT226Cat. No.: HY-13334ACAS No.: 915020-55-2Molecular Formula: CHFNOMolecular Weight: 534.53Target: PI3K; mTOR; AutophagyPathway: PI3K/Akt/mTOR; AutophagyStorage: Please store the product under the recommended conditions in the COA.BIOLOGICAL ACTIVITYDescription BGT226 (NVP-BGT226) is a PI3K (with
2、IC50s of 4 nM, 63 nM and 38 nM for PI3K, PI3K and PI3K)/mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells12.IC 24 hours) and both p-AKT Ser473 and p-mTOR Ser2448 are also decreased in BGT226-treated cell lines2.Cell Viability Assay2Cell Lin
3、e: FaDu cells; OECM1 cellsConcentration: 10, 100, 1000, 10000 nMIncubation Time:Result: Inhibited FaDu and OECM1 cells growth with IC50s of 23.17.4 and 12.55.1 nM, respectively.Western Blot Analysis2Cell Line: FaDu cells; OECM1 cellsConcentration: 200 nMIncubation Time: 24 hoursResult: p-mTOR Ser248
4、1 expression levels decreased, and both p-AKT Ser473 and p-mTOR Ser2448 expression levels also decreased.Product Data Sheet InhibitorsAgonistsScreening Librarieswww.MedChemE1In Vivo BGT226 (2.5 and 5 mg/kg; oral administration for 21 days in male athymic mice) causes 34.7% and 76.1% reduction of the
5、 tumor growth on day 21 compared with control2.Animal Model: Male athymic mice (strain BALB/cAnN.Cg-Foxn1nu/CrlNarl) with FaDu cell xenografted mouse model2Dosage: 2.5 and 5 mg/kgAdministration: Oral administration; 21 daysResult: Caused 34.7% and 76.1% reduction of the tumor growth.CUSTOMER VALIDAT
6、IONSee more customer validations on www.MedChemEREFERENCES1. 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 Sep;23(9):2399-408.2. Chang KY, et al.
7、 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 Nov 15;17(22):7116-26.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: techMedChemEAddress: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. Harvard Medical School LINCS LIBRARYwww.MedChemE2