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AZD6244 (ARRY-142886, Selumetinib) is a potent MEK 1/2 inhibitor with GI50 values ranging from 14 to 50 nM. AZD6244 has potential to inhibit proliferation and induce apoptosis and differentiation, but the response varies between different xenografts.
BMC Biol. 2021 May 20;19(1):108.
Very long intergenic non-coding (vlinc) RNAs directly regulate multiple genes in cis and trans
AZD6244 purchased from AbMole
Sci Rep. 2021 Jun 14;11(1):12497.
Neuroprotective effect of selumetinib on acrolein-induced neurotoxicity
AZD6244 purchased from AbMole
Cell Rep. 2019 Feb 5;1518-1532.e9.
Pre-existing Functional Heterogeneity of Tumorigenic Compartment as the Origin of Chemoresistance in Pancreatic Tumors.
AZD6244 purchased from AbMole
Apoptosis. 2018 May 18.
Down-regulating IL-6/GP130 targets improved the anti-tumor effects of 5-fluorouracil in colon cancer.
AZD6244 purchased from AbMole
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Source | Apoptosis (2018). Figure 6. AZD6244 (Abmole Bioscience. USA) |
| Method | Western Blot | |
| Cell Lines | HT29 and SW480 cells | |
| Concentrations | 32 μmol/l | |
| Incubation Time | 24 h | |
| Results | Resembling the WB results from the BZA treatment, the inhibitors AG490, NVP-BEZ23 and AZD6244 imitated BZA function, down-regulating the pivotal protein of the JAK/STAT3, PI3K/AKT/mTOR and Ras/Raf/MEK/ERK signal pathways |
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Source | Apoptosis (2018). Figure 5. AZD6244 (Abmole Bioscience. USA) |
| Method | cell apoptosis assay | |
| Cell Lines | HT29 and SW480 cells | |
| Concentrations | 32 μmol/l | |
| Incubation Time | 24 h | |
| Results | In addition, using the respective AG490 (50 μmol/l), NVP-BEZ235 (96 nmol/l) and AZD6244 (32 μmol/l) inhibitors for 24 h to mimic the BZA effect in colon cancer cells, we observed that the Bad/Bcl-2 ratio was significantly up-regulated and that Ki-67 mRNA expression was substantially down-regulated in this treatment group compared with the control group |
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Source | Cell Biol Int (2014). Figure 5. AZD6244 |
| Method | Western blots | |
| Cell Lines | Raji and MOLT-4 cells | |
| Concentrations | 10 μM | |
| Incubation Time | 48 h | |
| Results | Consistent with role in the growth inhibition, silencing of Bim decreases the AZD6244-induced apoptosis (Figure 5D) and abrogates AZD6244 induced G1 arrest (Figure 5E). |
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Source | Cell Biol Int (2014). Figure 1. AZD6244 |
| Method | apoptosis assay | |
| Cell Lines | Raji and MOLT4 cells | |
| Concentrations | 10 μM | |
| Incubation Time | 48 h | |
| Results | AZD6244 significantly blocked ERK phosphorylation in Raji and MOLT4 cells (Figure 1A). AZD6244 significantly inhibited proliferation of both Raji and MOLT4 in a dose-dependent manner (n¼3, P<0.01; Figure 1B). |
| Cell Experiment | |
|---|---|
| Cell lines | HT-29, Malme-3M, MIAPaCa-2, SK-MEL-2, SK-MEL-28, BxPC3, BT-474, Zr-75-1, Malme-3 |
| Preparation method | Cellular viability assays Cells plated in 96-well plates were incubated with multiple concentrations of compound for 3 days. The number of viable cells was determined using the CellTiter 96 Aqueous Nonradioactive Cell Proliferation Assay (Promega, Madison, WI). |
| Concentrations | 0-50µM |
| Incubation time | 3 days |
| Animal Experiment | |
|---|---|
| Animal models | HT-29 and BxPC3 xenograft |
| Formulation | 10% ethanol/10% cremophor EL/80% D5W |
| Dosages | 10, 25, 50, or 100 mg/kg BID |
| Administration | oral |
| Molecular Weight | 457.68 |
| Formula | C17H15BrClFN4O3 |
| CAS Number | 606143-52-6 |
| Solubility (25°C) | DMSO 30 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. |
| 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. |
| TAK-733
TAK-733 is a potent and selective MEK allosteric site inhibitor with IC50 of 3.2nM for the treatment of cancer. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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