NVP-BGT226

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NVP-BGT226 (BGT226) 是一种有效的双重 PI3K/mTOR 抑制剂，优先考虑 PI3Kα 和 mTOR。

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.

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.

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 modelDosage:2.5 and 5 mg/kg Administration:Oral administration; 21 days Result:Caused 34.7% and 76.1% reduction of the tumor growth.

BGT226 | NVP-BGT 226 | BGT-226

PI3K/Akt/mTOR signaling

PI3K

PI3Kα|PI3Kβ|PI3Kγ

Cancer

Solid Tumors

1245537-68-1

650.6

C32H29F3N6O6

>98% (HPLC)

10 mM in DMSO

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|

8-(6-methoxypyridin-3-yl)-3-methyl-1-(4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)-1H-imidazo[4,5-c]quinolin-2(3H)-one with maleic acid

(-20℃)

With Ice Pack

≥ 2 years