BGT226-maleate-NVP-BGT226-maleate-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBGT226 maleateCat. No.: HY-13334CAS No.: 1245537-68-1Synonyms: NVP-BGT226 (maleate)分式: CHFNO分量: 650.6作靶點: PI3K; mTOR; Autophagy作通路: PI3K/Akt/mTOR; Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解

2、性數(shù)據(jù)體外實驗 DMSO : 42.86 mg/mL (65.88 mM; Need ultrasonic)H2O : 90% corn oilSolubility: 2.5 mg/mL (3.84 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 BGT226 maleate (NVP-BGT226 maleate)種 PI3K (針對 PI3K，PI3K，PI3K 的IC50分別是4 nM，63nM，38 nM ) /mTOR 雙抑制劑，對頭頸癌細(xì)胞具有較強(qiáng)的

3、長抑制活性 1 2。IC50 & Target PI3K PI3K PI3K mTOR4 nM (IC50) 38 nM (IC50) 63 nM (IC50)Autophagy體外研究 BGT226 shows significant growth inhibition or signal blockage profiles compared with LY294002 andRapamycin. BGT226 (10-10000 nM) inhibits FaDu and OECM1 cells growth with IC50s of 23.17.4 and12.55.1 nM, res

4、pectively 2.The expression levels of p-mTOR Ser2481 are decreased in BGT226-treated cell lines (200 nM; 24 hours)and both p-AKT Ser473 and p-mTOR Ser2448 are also decreased in BGT226-treated cell lines 2.Cell Viability Assay 2Cell Line: FaDu cells; OECM1 cellsConcentration: 10, 100, 1000, 10000 nMIn

5、cubation Time:Result: Inhibited FaDu and OECM1 cells growth with IC50s of 23.17.4 and 12.55.1 nM,respectively.Western Blot Analysis 2Cell Line: FaDu cells; OECM1 cellsConcentration: 200 nMIncubation Time: 24 hourResult: p-mTOR Ser2481 expression levels decreased, and both p-AKT Ser473 and p-mTORSer2

6、448 expression levels also decreased.體內(nèi)研究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 tumor growth on day 21 compared with control 2.Animal Model: Male athymic mice (strain BALB/cAnN.Cg-Foxn1nu/CrlNarl) with FaDu cell xenograft

7、edmouse model 2Dosage: 2.5 and 5 mg/kgAdministration: Oral administration; 21 days2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEResult: Caused 34.7% and 76.1% reduction of the tumor growth.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. Harvard Medical School LINCS LIBRARYSee more

8、 customer validations on HYPERLINK / www.MedChemEREFERENCES1. Markman B, et al. Phase I safety, pharmacokinetic, and pharmacodynamic study of the oral phosphatidylinositol-3-kinase and mTORinhibitor BGT226 in patients with advanced solid tumors. Ann Oncol. 2012 Sep;23(9):2399-408.2. Chang KY, et al. Novel phosphoinositide 3-kinase/mTOR dual inhibitor, NVP-BGT226, displays potent growth-inhibitory activity againsthuman head and neck cancer cells in vitro and in vivo. Clin Cancer Res. 2011 Nov 15;17(22):7116-26.McePdfHeightCaution: Product has not been fully validated for medical a