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.
Cited by 6 Publications
5 Customer Reviews
(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.
Purity & Quality Control
Choose Selective MEK Inhibitors
|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)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.