BGT226 (NVP-BGT226 maleate) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ) /mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells.
IC50&Target
PI3Kα
4 nM (IC50)
PI3Kβ
63 nM (IC50)
PI3Kγ
38 nM (IC50)
mTOR
Autophagy
体外研究
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.
体内研究
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.
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.
分子式
C28H25N6O2F3.C4H4O4
分子量
650.60
CAS号
1245537-68-1
运输条件
Room temperature in continental US; may vary elsewhere.