NVP-BGT226
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
- BGT226
- NVP-BGT226
- CAS:
- 1245537-68-1
- MF:
- C28H25F3N6O2.C4H4O4
- MW:
- 650.6044696
- 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-BGT226Supplier
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