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| | NVP-BGT226 Basic information |
| Product Name: | NVP-BGT226 | | Synonyms: | 8-(6-methoxypyridin-3-yl)-3-methyl-1-(4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)-1H-imidazo[4,5-c]quinolin-2(3H)-one Maleic acid;BGT-226 maleate;BGT226 (NVP-BGT226);BGT226 (NVP-BGT226);NVP-BGT226;8-(6-Methoxypyridin-3-yl)-3-methyl-1-(4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)-1H-imidazo;1-(3-(Trifluoromethyl)-4-(piperazin-1-yl)phenyl)-8-(6-methoxypyridin-3-yl)-3-methyl-1H-imidazo[4,5-c]quinolin-2(3H)-one maleic acid salt;NVP-BGT226;NVP-BGT226 (BGT226) | | CAS: | 1245537-68-1 | | MF: | C28H25F3N6O2.C4H4O4 | | MW: | 650.6044696 | | EINECS: | | | Product Categories: | Akt;mTOR;PI3K;PI3K/Akt/mTOR;Inhibitors | | Mol File: | 1245537-68-1.mol |  |
| | NVP-BGT226 Chemical Properties |
| Melting point | >215°C (dec.) | | storage temp. | Hygroscopic, -20°C Freezer, Under inert atmosphere | | solubility | DMSO (Slightly) | | form | Solid | | color | White to Pale Yellow |
| | NVP-BGT226 Usage And Synthesis |
| Uses | BGT 226 is a novel phosphatidyl inositol-3 kinase/mammalian target of rapamycin (PI3K/mTOR ) dual inhibitor which has shown to be effective with gefitinib in epidermal growth factor receptor (EGFR) inhibitor-sensitive non-small cell lung cancer (NSCLC) therapy. | | Definition | ChEBI: BGT226 is the maleate salt of 8-(6-methoxypyridin-3-yl)-3-methyl-1-[4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl]-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one. 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 contains 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. |
| | target | PI3Kα | | IC 50 | PI3Kα: 4 nM (IC50); PI3Kγ: 38 nM (IC50); PI3Kβ: 63 nM (IC50); mTOR; Autophagy |
| | NVP-BGT226 Preparation Products And Raw materials |
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