BGT226 (NVP-NVP-BGT226) 是一种 PI3K（对于 PI3Kα；、PI3K&7#946；和 PI3Kγ；的 IC50 分别为 4 nM、63 nM 和 38 nM；）/mTOR 双重抑制剂，对人类头颈癌具有有效的生长抑制活性细胞。
| Cas No. | 1245537-68-1 |
| 别名 | NVP-BGT226 maleate |
| 化学名 | (Z)-but-2-enedioic acid;8-(6-methoxypyridin-3-yl)-3-methyl-1-[4-piperazin-1-yl-3-(trifluoromethyl)phenyl]imidazo[4,5-c]quinolin-2-one |
| Canonical SMILES | CN1C2=CN=C3C=CC(=CC3=C2N(C1=O)C4=CC(=C(C=C4)N5CCNCC5)C(F)(F)F)C6=CN=C(C=C6)OC.C(=CC(=O)O)C(=O)O |
| 分子式 | C28H25F3N6O2.C4H4O4 |
| 分子量 | 650.6 |
| 溶解度 | ≥ 16.275mg/mL in DMSO with gentle warming |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | BGT226 (NVP-BGT226) is a novel inhibitor of PI3K/mTOR for PI3Kα/β/γ with IC50 of 4 nM/63 nM/38 nM. [1]
The phosphatidylinositol-3-kinase (PI3K) pathway is one of the most commonly activated signaling pathways in pancreatic cancer and is a target of interest for new therapeutic approaches.
NVP-BGT226 is a novel dual class PI3K/mammalian target of rapamycin (mTOR) inhibitor. When used NVP-BGT226, cell viability decreased within 24-72 h after exposure to about 50% compared to untreated control cells in a concentration- but not time-dependent manner. [1] The dual PI3K/mTOR inhibitor NVP-BGT226 induces G0/G1 arrest and acts partially via downregulation of Survivin. NVP-BGT226 potently inhibited growth activity of cell lines, including SCC4, TU183 and KB cell lines with the IC50 ranging from 7.4 to 30.1 nM. [2]
In a FaDu cell xenografted mouse model, BGT226 inhibited tumor growth in a dose-dependent manner in a FaDu cell xenografted mouse model. Oral administration of BGT226 at 2.5 and 5 mg/kg for 3 weeks caused 34.7% and 76.1% reduction of the tumor growth on day 21, respectively (compared with control). BGT226 displayed comparable inhibition against tumor growth to rapamycin. The final volume of both groups was significantly smaller than those treated with LY294002 or the control. [2]
References:
[1]. Glienke, W, et al. The dual PI3K/mTOR inhibitor NVP-BGT226 induces cell cycle arrest and regulates Survivin gene expression in human pancreatic cancer cell lines. TUMOR BIOLOGY, 2014, 33(3): 757-765.
[2]. Chang KY, et al. Novel phosphoinositide 3-kinase/mTOR dual inhibitor, NVP-BGT226, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo. Clin Cancer Res, 2011, 17(22): 7116-7126. |
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