Free shipping on all orders over $ 500

TAK-733

Cat. No. M1750
TAK-733 Structure
Size Price Availability Quantity
10mg USD 220 In stock
50mg USD 670 In stock
100mg USD 900 In stock
Bulk Inquiry?

Quality Control
Biological Activity

TAK-733 is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity. MEK inhibitor TAK-733 selectively binds to and inhibits the activity of MEK1/2, preventing the activation of MEK1/2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK1/2 (MAP2K1/K2) are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK pathway and are often upregulated in a variety of tumor cell types.

Protocol
Cell Experiment
Cell lines a panel of CRC cell lines
Preparation method The antiproliferative effects of TAK-733 against CRC cell lines were determined using the sulforhodamine B (SRB) method. Briefly, cells in logarithmic growth phase were transferred to 96-well flat-bottomed plates with lids. Cell suspensions (100 μL) containing 3,000 to 5,000 viable cells were plated into each well and incubated overnight before exposure with increasing concentrations of TAK-733 for 72 hours. After treatment, medium was removed and the cells were fixed with cold 10% TCA for 30 minutes at 4°C. The cells were then washed with water and stained with 0.4% SRB (Fisher Scientific) for 30 minutes at room temperature and washed again with 1% acetic acid followed by stain solubilization with 10 mmol/L of Tris at room temperature. The plate was then read on a 96-well plate reader (Biotek Synergy 2) set at an absorbance wavelength of 565 nm. Cell proliferation curves were derived from the raw absorbance data and expressed as the percentage of vehicle-treated controls.
Concentrations 0~1µM
Incubation time 72 h
Animal Experiment
Animal models Patient-derived tumor explant models
Formulation 0.5% methylcellulose
Dosages 1 mg/kg once daily
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 504.23
Formula C17H15F2IN4O4
CAS Number 1035555-63-5
Purity 100.00%
Solubility DMSO ≥101 mg/mL
Storage at -20°C
References

BRAF L597 mutations in melanoma are associated with sensitivity to MEK inhibitors.
Dahlman et al. Cancer Discov. 2012 Jul 13. PMID: 22798288.

Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer.
Dong et al. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1315-9. PMID: 21310613.

Related MEK Products
BI-847325

BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively.

LY2801653

LY2801653 is a potent, orally bioavailable, small-molecule inhibitor of c-MET kinase(Ki= 2 nM).

Refametinib

Refametinib (BAY 86-9766, RDEA119) is a potent, highly selective and ATP non-competitive inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively.

GDC-0973

GDC-0973 is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase (MEK1/2).

PD 198306

PD 198306 is a cell-permeable and highly selective MEK inhibitor with IC50 of 8 nM.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: TAK-733 supplier, MEK, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.