BGT226 free base

SKU: orb1217478

Description

Bgt226 is a novel dual PI3K / mTOR inhibitor, it acts on PI3K α/β/γ with IC50 of 4 nM / 63 nM / 38 nM, respectively.

Key Properties

• CAS Number: 915020-55-2
• MW: 534.53
• Purity: >98% (HPLC)
• Formula: C₂₈H₂₅F₃N₆O₂
• SMILES: CN(c(cnc(c1c2)ccc2-c(cc2)cnc2OC)c1N1c(cc2)cc(C(F)(F)F)c2N2CCNCC2)C1=O
• Target: PI3K
• Solubility: In Vitro: DMSO : 10 mg/mL (18.71 mM)

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 hours. 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

NVP-BGT226

Quick Database Links

Gene Symbol

PI3K