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TAK-733 is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity. MEK inhibitor TAK-733 selectively binds to and inhibits the activity of MEK1/2, preventing the activation of MEK1/2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK1/2 (MAP2K1/K2) are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK pathway and are often upregulated in a variety of tumor cell types.
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Source | Oncotarget (2015). Figure 2. TAK-733 |
| Method | Immunoblotting analysis | |
| Cell Lines | CRC cell lines | |
| Concentrations | 1.25 uM | |
| Incubation Time | 2 h | |
| Results | The effects of TAK-733 on the modulation of downstream targets in the MAPK and PI3K pathways were analyzed in 2 sensitive and 4 resistant cell lines |
| Cell Experiment | |
|---|---|
| Cell lines | a panel of CRC cell lines |
| Preparation method | The antiproliferative effects of TAK-733 against CRC cell lines were determined using the sulforhodamine B (SRB) method. Briefly, cells in logarithmic growth phase were transferred to 96-well flat-bottomed plates with lids. Cell suspensions (100 μL) containing 3,000 to 5,000 viable cells were plated into each well and incubated overnight before exposure with increasing concentrations of TAK-733 for 72 hours. After treatment, medium was removed and the cells were fixed with cold 10% TCA for 30 minutes at 4°C. The cells were then washed with water and stained with 0.4% SRB (Fisher Scientific) for 30 minutes at room temperature and washed again with 1% acetic acid followed by stain solubilization with 10 mmol/L of Tris at room temperature. The plate was then read on a 96-well plate reader (Biotek Synergy 2) set at an absorbance wavelength of 565 nm. Cell proliferation curves were derived from the raw absorbance data and expressed as the percentage of vehicle-treated controls. |
| Concentrations | 0~1µM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | Patient-derived tumor explant models |
| Formulation | 0.5% methylcellulose |
| Dosages | 1 mg/kg once daily |
| Administration | oral gavage |
| Molecular Weight | 504.23 |
| Formula | C17H15F2IN4O4 |
| CAS Number | 1035555-63-5 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related MEK Products |
|---|
| AS703026
Pimasertib (AS-703026) is a novel selective MEK1/2 inhibitor, and induces pleiotropic anti-myeloma activity in vitro and in vivo. |
| AZD6244
AZD6244 (ARRY-142886, Selumetinib) is a potent MEK 1/2 inhibitor with GI50 values ranging from 14 to 50 nM. |
| AZD8330
AZD8330 (ARRY-424704) is a novel, selective, highly efficacious, uncompetitive MEK inhibitor with an IC50 of 7 nM. |
| CI-1040
CI-1040 (PD184352) is a targeted signal transduction inhibitor of MEK with a ki value of 300nM in vitro. |
| ARRY-162 (Binimetinib)
ARRY-162 (MEK-162; Binimetinib) is a selective, potent inhibitor of MEK and cellular pERK with IC50 of 12 nM and 11 nM, respectively. |
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