Home MAPK MEK inhibitor TAK-733 For research use only.

TAK-733

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 Chemical Structure

TAK-733 Chemical Structure

CAS No. 1035555-63-5

Purity & Quality Control

TAK-733 Related Products

Signaling Pathway

MEK Signaling Pathways

MEK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
COLO205 Cytotoxicity assay 72 hrs Cytotoxicity against human COLO205 cells after 72 hrs by MTS assay, EC50=0.0021μM. 21310613
A375 Cytotoxicity assay 72 hrs Cytotoxicity against human A375 cells after 72 hrs by MTS assay, EC50=0.0031μM. 21310613
COLO205 Function assay Inhibition of MEK1 in human COLO205 cells, IC50=0.00692μM. 24755426
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
Click to View More Cell Line Experimental Data

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
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]
Experimental Result Images Methods Biomarkers Images PMID
Growth inhibition assay Cell viability 26918363
Western blot p-ERK / p-AKT / p-S6R / p-GSK3 pRb / Cyclin E 26918363
In Vivo
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]
Animal Research 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.
Dosages 10 mg/kg
Administration Orally administrated once daily for 21 days
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

Chemical Information & Solubility

Molecular Weight 504.23 Formula

C17H15F2IN4O4
CAS No. 1035555-63-5 SDF Download TAK-733 SDF
Smiles CN1C2=C(C(=C(C1=O)F)NC3=C(C=C(C=C3)I)F)C(=O)N(C=N2)CC(CO)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 101 mg/mL ( (200.3 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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

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