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915020-55-2

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915020-55-2 Structure

915020-55-2 Structure
IdentificationBack Directory
[Name]

BGT226
[CAS]

915020-55-2
[Synonyms]

BGT-226 free base
8-(6-Methoxypyridin-3-yl)-3-methyl-1-[4-(piperazin-1-yl)-3-trifluoromethylphenyl]-1,3-dihydroimidazo[4,5-c]quinolin-2-one
2H-Imidazo[4,5-c]quinolin-2-one, 1,3-dihydro-8-(6-methoxy-3-pyridinyl)-3-methyl-1-[4-(1-piperazinyl)-3-(trifluoromethyl)phenyl]-
[Molecular Formula]

C28H25F3N6O2
[MDL Number]

MFCD22376639
[MOL File]

915020-55-2.mol
[Molecular Weight]

534.53
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[solubility ]

Soluble in DMSO
[form ]

Solid
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

8-(6-Methoxypyridin-3-yl)-3-methyl-1-(4-piperazin-1-yl)-3-(trifluoromethyl)phenyl-1H-imidazol[4,5-c]quinolin-2(3H)-one is an intermediate used in the screening of anti-prostate cancer drug targeting PI3K-AKT-mTOR pathway.
[Definition]

ChEBI: BGT226 free base is an imidazoquinoline that is 3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinoline substituted at position 1 by a 3-trifluoromethyl-4-(piperazin-1-yl)phenyl group and at position 8 by a 6-methoxypyridin-3-yl group. A dual PI3K/mTOR inhibitor. It has a role as an antineoplastic agent, a mTOR inhibitor and an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor. It is an imidazoquinoline, a N-arylpiperazine, a member of pyridines, an organofluorine compound and an aromatic ether. It is a conjugate base of a BGT226(1+).
[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[2].

Animal Model:Male athymic mice (strain BALB/cAnN.Cg-Foxn1nu/CrlNarl) with FaDu cell xenografted mouse model[2]
Dosage:2.5 and 5 mg/kg
Administration:Oral administration; 21 days
Result:Caused 34.7% and 76.1% reduction of the tumor growth.
[IC 50]

PI3Kα: 4 nM (IC50); PI3Kβ: 63 nM (IC50); PI3Kγ: 38 nM (IC50); mTOR; Autophagy
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