TAK-733

Catalog No.S2617

TAK-733 Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 340 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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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.

  • After starved in serum-free medium for 24 h, T47D cells incubated with the indicated concentrations of TAK-733 for 3 h,followed by 20-minute stimolation of 100ng/ml EGF.

    Dr. Zhang of Tianjin Medical University. TAK-733 purchased from Selleck.

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Biological Activity

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.
Targets
MEK1 [1]
(Cell-free assay)
3.2 nM
In vitro

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. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
COLO205 cells MXXDfZRwfG:6aXPpeJkh[XO|YYm= MVi3NkBp M{D4XGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNQVE9{MEWgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiRVO1NF0xNjByMkGg{txO NH;EUoozOTNzME[xNy=>
A375 cells NUCwfllIS3m2b4TvfIlkcXS7IHHzd4F6 MXu3NkBp M174[GN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE{PzViY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VWyCjc4PhfUwhTUN3ME2zMlEhdk1? MY[yNVMyODZzMx?=

... Click to View More Cell Line Experimental Data

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. [1] TAK-733 shows maximally efficacious doses at once daily orally doses of 10 mg/kg. [2]

Protocol

Animal Research:[2]
+ Expand
  • Animal Models: Human solid tumor xenograft models including NSCLC (NCI H23 [KRAS and LKB1 mutations]), CRC (SW620 [KRAS, APC, p53 mutations]) Pancreatic cancer (Panc 1 and Capan 1 [KRAS mutations] and BxPC-3 [No MAPK mutations]) models in immunocompromised mice.
  • Formulation: Saline
  • Dosages: 10 mg/kg
  • Administration: Orally administrated once daily for 21 days
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 101 mg/mL (200.3 mM)
Water Insoluble
Ethanol Insoluble

* 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.

Chemical Information

Molecular Weight 504.23
Formula

C17H15F2IN4O4

CAS No. 1035555-63-5
Storage powder
Synonyms N/A

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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

Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID