NVP-BGT226

SKU: orb1226685

Description

NVP-BGT226 (BGT226) is a potent, dual PI3K/mTOR inhibitor with a preference for PI3Kα (wild type and mutated) and mTOR ( PI3Kα, PI3Kβ and PI3Kγ, IC50=4, 63 and 38 nM); displays potent antiproliferative activity against various human head and neck cancer cell lines in vitro (IC50=7.4-30.1 nM), downregulates the expression levels of the downstream proteins p-p70S6K and p-4E-BP1 in cells, induces cell-cycle arrest at the G0-G1 phase at 60 nM; BGT226 significantly delays tumor growth in a dose-dependent manner, along with suppressed cytoplasmic expression of p-p70S6K and the presence of autophagosome formation in xenografted animal modes.Solid Tumors Discontinued(In Vitro):BGT226 shows significant growth inhibition or signal blockage profiles compared with LY294002 and Rapamycin. BGT226 (10-10000 nM) inhibits FaDu and OECM1 cells growth with IC50s of 23.1±7.4 and 12.5±5.1 nM, respectively .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.(In 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 tumor growth on day 21 compared with control.

Key Properties

• CAS Number: 1245537-68-1
• MW: 650.6
• Purity: >98% (HPLC)
• Formula: C₃₂H₂₉F₃N₆O₆
• SMILES: OC(=O)\C=C/C(O)=O.COC1=CC=C(C=N1)C1=CC=C2N=CC3=C(N(C(=O)N3C)C3=CC=C(N4CCNCC4)C(=C3)C(F)(F)F)C2=C1 |c:11,13,20,41,49,t:9,16,18,22,30,32|
• Target: PI3K
• Solubility: 10 mM in DMSO

Bioactivity

• In 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 tumor growth on day 21 compared with control. Animal model: Male athymic mice (strain BALB/cAnN. Cg-Foxn1nu/CrlNarl) with FaDu cell xenografted mouse model. Dosage: 2.5 and 5 mg/kg. Administration: Oral administration; 21 days. Result: Caused 34.7% and 76.1% reduction of the tumor growth.
• In Vitro:
  BGT226 shows significant growth inhibition or signal blockage profiles compared with LY294002 and Rapamycin. BGT226 (10-10000 nM) inhibits FaDu and OECM1 cells growth with IC50s of 23.1±7.4 and 12.5±5.1 nM, respectively. 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. Cell Viability Assay Cell line: FaDu cells; OECM1 cells. Concentration: 10, 100, 1000, 10000 nM. Incubation time: Result: Inhibited FaDu and OECM1 cells growth with IC50s of 23.1±7.4 and 12.5±5.1 nM, respectively. Western blot analysis. Cell line: FaDu cells; OECM1 cells. Concentration: 200 nM. Incubation time: 24 hour. Result: p-mTOR Ser2481 expression levels decreased, and both p-AKT Ser473 and p-mTOR Ser2448 expression levels also decreased.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BGT226 | NVP-BGT 226 | BGT-226

Quick Database Links

Gene Symbol

PI3K