Molecular Weight(MW): 504.23
TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc. Phase 1.
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(c) Fold induction of apoptotic cells after 3-day compound or vehicle (DMSO) treatment, as measured by annexin V positivity. Error bars indicate s.d.'s (n=4). **P<0.01, ***P<0.001, two-way ANOVA with Holm Sidak multiple comparisons correction.
Nat Commun, 2016, 7:13701.. TAK-733 purchased from Selleck.
Both PI3K/Akt and MAPK signaling pathways are essential in lung cancer cells harboring wild-type EGFR (A) PI3K inhibition suppressed proliferation of lung cancer cells harboring mutant or wild-type EGFR. A549 and PC-9 cells were incubated in the presence of various concentrations of GSK2126458 or PF04691502. Cell extracts were prepared after 1 h of treatment and immunoblotted with the indicated antibodies (upper panel). Cell growth was measured by MTT assay after 72 h (lower panel). (B) MEK inhibition suppressed proliferation of lung cancer cells harboring mutant or wild-type EGFR. A549 and PC-9 cells were incubated in the presence of various concentrations of AZD-8330 or TAK-733. Cell extracts were prepared after 1 h of treatment and immunoblotted with the indicated antibodies (upper panel). Cell growth was measured by MTT assay after 72 h (lower panel).
Oncotarget, 2016, 7(13):16273-81.. TAK-733 purchased from Selleck.
Effect of MEK inhibitor TAK-733 in A549 cells. A549 cells were incubated with increasing concentrations of TAK-733 for 2 h. The cell lysates were harvested and phosphorylation of indicated proteins was determined by Western blotting.
Dr.Wang from Southern Medical Hospital . TAK-733 purchased from Selleck.
Mouse carcinoma cells were treated with the inhibitors for 16 and 40 h at the concentrations indicated. The effect on S-phase was evident at 16 hrs. (A) whereas apoptosis was induced at 40h. (B) Biological effects of the compounds correlated with effects on phosphorylation of the MEK target ERK. (C) IC50 on S-phase and ERK-posphorylation: TAK-733=1-10nM, GSK1120212=<1nM.
Jonas Nilsson, PhD from University of Gothenburg. TAK-733 purchased from Selleck.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|Description||TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc. Phase 1.|
TAK-733 is highly potent and selective MEK allosteric site inhibitor with IC50 of 3.2 nM. TAK-733 shows potent enzymatic and cell activity with an EC50 of 1.9 nM against ERK phosphorylation in cells. 
|In vivo||TAK-733 demonstrates broad antitumor activity in mouse xenograft models of human cancer including models of melanoma, colorectal, NSCLC, pancreatic and breast cancer. TAK-733 is well tolerated with pharmacokinetics and pharmacodynamics that support once-daily oral dosing in humans.  TAK-733 shows maximally efficacious doses at once daily orally doses of 10 mg/kg. |
|In vitro||DMSO||101 mg/mL (200.3 mM)|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01613261||Withdrawn||Advanced Nonhematologic Malignancies||Millennium Pharmaceuticals, Inc.||August 2013||Phase 1|
|NCT00948467||Completed||Advanced Non-hematologic Malignancies|Advanced Metastatic Melanoma||Millennium Pharmaceuticals, Inc.||December 2009||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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