BGT226 free base

Research use only, not for human use.

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.

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.

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.

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.

NVP-BGT226

PI3K/Akt/mTOR signaling

PI3K

PI3Kα| PI3Kβ| PI3Kγ| mTOR

——

——

915020-55-2

534.53

C28H25F3N6O2

>98% (HPLC)

In Vitro:?DMSO : 10 mg/mL (18.71 mM)

CN(c(cnc(c1c2)ccc2-c(cc2)cnc2OC)c1N1c(cc2)cc(C(F)(F)F)c2N2CCNCC2)C1=O

——

(-20℃)

With Ice Pack

≥ 2 years