BEZ235 (NVP-BEZ235) is a potent dual inhibitor of PI3K and mTOR. BEZ235 (NVP-BEZ235) is able to effectively and specifically block the dysfunctional activation of the PI3K pathway and induce G (1) arrest. It also inhibits the growth of human cancer in animal models. For Class I PI3K family, NVP-BEZ235 biochemical IC50 are 4nM against p110α, 75nM against p110β, 7nM against p110σ, 5nM against p110γ.
J Stroke Cerebrovasc Dis. 2023 Jan 16;32(3):106984.
Inhibition of PI3K/Akt/mTOR signaling by NDRG2 contributes to neuronal apoptosis and autophagy in ischemic stroke
BEZ235 purchased from AbMole
Cell Reports. 2019 Feb 5;1518-1532.e9.
Pre-existing Functional Heterogeneity of Tumorigenic Compartment as the Origin of Chemoresistance in Pancreatic Tumors.
BEZ235 purchased from AbMole
Cancer Biol Ther. 2018 May 25;1-20.
Preclinical evaluation of novel PI3K/mTOR dual inhibitor SN202 as potential anti-renal cancer agent
BEZ235 purchased from AbMole
Apoptosis. 2018 May 18.
Down-regulating IL-6/GP130 targets improved the anti-tumor effects of 5-fluorouracil in colon cancer.
BEZ235 purchased from AbMole
Cell Death and Disease. 2018 Jan 26;9:137-52.
Downregulation of MCL-1 and upregulation of PUMA using mTOR inhibitors enhance antitumor efficacy of BH3 mimetics in triple-negative breast cancer
BEZ235 purchased from AbMole
Cell Experiment | |
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Cell lines | MKN45, BT474, SNU216 and NCI-N87 cell lines |
Preparation method | Cell viability assay Cells were seeded at a density of 2000 cells per well in a 96-well plate and incubated overnight in complete medium. Cells were treated with either trastuzumab, BEZ235, Everolimus, AZD6244 alone, or trastuzumab combined with BEZ235 or Everolimus or AZD6244. After 72 h of incubation, cell viability was determined using the MTS tetrazolium substrate (CellTiter 96 Aqueous One Solution Cell Proliferation Assay, Promega, Madison, WI, USA) following the manufacturer’s instructions. The absorbance was measured at 490 nm using a spectrophotometer. All experiments were repeated three times with at least triplicate readings for each concentration. |
Concentrations | 0~800nM |
Incubation time | 72h |
Animal Experiment | |
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Animal models | Xenograft models in non-obese diabetic/severe combined immunodeficiency (NOD/SCID) mice |
Formulation | BEZ235 was formulated in 0.9 % NaCl as a homogeneous suspension (9 mg/mL) and stored at 4 °C until further use in the in vivo experiments. |
Dosages | 45 mg/kg body weight, daily |
Administration | oral gavage |
Molecular Weight | 469.55 |
Formula | C30H23N5O |
CAS Number | 915019-65-7 |
Solubility (25°C) | DMSO 3 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts.The Ki of PF-06843195 acting on PI3Kα and PI3Kδ is less than 0.018 nM and 0.28 nM, respectively.PF-06843195 has a significant inhibitory effect on PI3K/mTOR signaling pathway and had a long-lasting anti-tumor effect. |
AZD8154
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ME-401
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3-Hydroxyanthranilic acid
3-Hydroxyanthranilic Acid (3-HAA, 3-HANA), a tryptophan metabolite, has an immunomodulatory effect that may result from inhibition of PI3K/Akt/mTOR and NF-κB activity, thereby decreasing the production of pro-inflammatory mediators. |
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