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AZD6244 (Selumetinib)

Catalog No. S1008 5 5 12 Customer Review(s) Product Citations45 Product Citation(s)
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AZD6244 (Selumetinib) Chemical Structure

Bio Information

Activating mutations in the BRAF gene, primarily at V600E, are associated with poorer outcomes in patients with papillary thyroid cancer. MAPK kinase (MEK), immediately downstream of BRAF, is a promising target for ras-raf-MEK-ERK pathway inhibition. In addition to thyroid cancer, BRAF-activating mutations are prevalent in melanoma (-59%), colorectal cancer (5–22%), serous ovarian cancer (-30%), and several other tumor types. [1]
Four lines bearing V600E BRAF mutations were all sensitive to AZD6244, with GI50 values ranging from 14 to 50 nM. A positive control BRAF mutant melanoma line, SKMel28, [2]exhibited a similar GI50 of 23 nM.

References:

[1] NATURE 27 JUNE 2002;417：949－954

[2] NATURE 19 January 2006;439：358－362

Chemical Information

Molecular Weight (WM): 457.68
Formula:

C17H15BrClFN4O3
Solubility(R.T.:25°C): DMSO 92mg/mL 
Water <1mg/mL 
Ethanol <1mg/mL 

Quality Control

View current batch:
H-NMR HPLC H-NMR HPLC H-NMR HPLC H-NMR HPLC H-NMR HPLC H-NMR HPLC H-NMR HPLC H-NMR HPLC

Research Area

MAPK >> MEK >> MEK Inhibitors

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Related Antibodies

Information  
Reactivity: 薛亚红

AZD6244 (Selumetinib) has been referenced in 45 publications.

Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors.
Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation.
COT drives resistance to RAF inhibition through MAP kinase pathway reactivation.
Exome sequencing identifies recurrent somatic MAP2K1 and MAP2K2 mutations in melanoma.
Exon capture analysis of G protein-coupled receptors identifies activating mutations in GRM3 in melanoma.
MED12 controls the response to multiple cancer drugs through regulation of TGF-β receptor signaling.
Effect of SMURF2 Targeting on Susceptibility to MEK Inhibitors in Melanoma.
Intestinal renin-angiotensin system is stimulated after deletion of Lkb1.
MEK1 mutations confer resistance to MEK and B-RAF inhibition.
Strong negative feedback from Erk to Raf confers robustness to MAPK signalling
BH3-only protein silencing contributes to acquired resistance to PLX4720 in human melanoma.
Combinatorial treatments that overcome PDGFRβ-driven resistance of melanoma cells to V600EB-RAF inhibition.
Activation of FOXO3a is sufficient to feverse mitogen-activated protein/extracellular signal-regulated kinase kinase inhibitor chemoresistance in human cancer.
Actin and ERK1/2-CEBPβ signaling mediates phagocytosis-induced innate immune response of osteoprogenitor cells.
Characteristics of lung cancers harboring NRAS mutations.
MicroSCALE screening reveals genetic modifiers of therapeutic response in melanoma.
Vertical targeting of the phosphatidylinositol-3 kinase pathway as a strategy for treating melanoma.
The Akt inhibitor MK2206 synergizes, but Perifosine antagonizes, the BRAFV600E inhibitor PLX4032 and the MEK1/2 inhibitor AZD6244 in the inhibition of thyroid cancer cells.
p37δ is a new isoform of PI3K p111δ that increases cell proliferation and is overexpressed in tumors.
p53 rescue through HDM2 antagonism suppresses melanoma growth and potentiates MEK inhibition.
Treatment with selumetinib preserves cardiac function and improves survival in cardiomyopathy caused by mutation in the lamin A/C gene
Oncogenic MAP2K1 mutations in human epithelial tumors.
Selective Cox-2 inhibitor celecoxib induces epithelial-mesenchymal transition in human lung cancer cells via activating MEK-ERK signaling.
Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor.
A genome-scale RNA interference screen implicates NF1 loss in resistance to RAF inhibition.
Down-regulation of mitogen-inducible gene 6, a negative regulator of EGFR, enhances resistance to MEK inhibition in KRAS mutant cancer cells.
Blockade of the MEK/ERK signalling cascade by AS703026, a novel selective MEK1/2 inhibitor, induces pleiotropic anti-myeloma activity in vitro and in vivo.
SHOC2 and CRAF Mediate ERK1/2 Reactivation in Mutant NRAS-mediated Resistance to RAF Inhibitor.
Small molecule inhibition of the steroid receptor coactivators, SRC-3 and SRC-1.
Glucose regulates cyclin D2 expression in quiescent and replicating pancreatic β-cells through glycolysis and calcium channels.
Sorafenib and Mek inhibition is synergistic in medullary thyroid carcinoma in vitro.
FOXD3 regulates migration properties and Rnd3 expression in melanoma cells.
An In Vivo C. elegans Model System for Screening EGFR-Inhibiting Anti-Cancer Drugs.
K-RAS mutant pancreatic tumors show higher sensitivity to MEK than to PI3K inhibition in vivo.
Reversing melanoma cross-resistance to BRAF and MEK inhibitors by co-targeting the AKT/mTOR pathway.
The protein kinase C inhibitor enzastaurin exhibits antitumor activity against uveal melanoma.
Involvement of epidermal growth factor receptor signaling in estrogen inhibition of oocyte maturation mediated through the G protein-coupled estrogen receptor (Gper) in zebrafish (Danio rerio).
Aggravation of Inflammatory Response by Co-Stimulation with Titanium Particles and Mechanical Perturbations in Osteoblast- and Macrophage- like Cells.
Selective inhibition of extracellular signal-regulated kinases 1/2 blocks nerve growth factor to brain-derived neurotrophic factor signaling and suppresses the development of and reverses already established pain behavior in rats.
Autophagic activation potentiates the antiproliferative effects of tyrosine kinase inhibitors in medullary thyroid cancer.
Preexisting MEK1 Exon 3 mutations in V600E/KBRAF melanomas do not confer resistance to BRAF inhibitors.
Modeling of lamin A/C mutation premature cardiac aging using patient‐specific induced pluripotent stem cells.
Inhibition of metadherin sensitizes breast cancer cells to AZD6244
Simultaneous exposure of transformed cells to SRC family inhibitors and CHK1 inhibitors causes cell death.
Detection of Allosteric Kinase Inhibitors by Displacement of Active Site Probes.

We have 12 customer reviews of AZD6244 (Selumetinib).

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Average Customer Review

(12 customer reviews)

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  • ;Oncogene, 2012, 31, 3277–3286
    AZD6244 (Selumetinib) purchased from Selleck


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  • ;Nat Genet, 2011, 43(11), 1119-26.
    AZD6244 (Selumetinib) purchased from Selleck


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  • Data from [Cancer Res 2010;70, 4709-4718]
    AZD6244 (Selumetinib) purchased from Selleck


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  • Data from [Br J Haematol 2010;149, 537–549]
    AZD6244 (Selumetinib) purchased from Selleck


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  • ;Dr Jong-In Park of Medical College of Wisconsin
    AZD6244 (Selumetinib) purchased from Selleck


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  • Data from [Cancer Res 2010;70, 4709-4718]
    AZD6244 (Selumetinib) purchased from Selleck


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  • Data from [Nature 2010;468, 968-972]
    AZD6244 (Selumetinib) purchased from Selleck


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  • Data from [PNAS 2009;106, 20411-20416]
    AZD6244 (Selumetinib) purchased from Selleck


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  • Data from [Clin Cancer Res 2010;16, 6029-6039]
    AZD6244 (Selumetinib) purchased from Selleck


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  • Data from [NATURE 2010;468, 973-977]
    AZD6244 (Selumetinib) purchased from Selleck

  •   
  • it is great to hear from you and I am very happy to work with you and selleck. From our experience all the inhibitors works very well and we are very satisfied with the quality of the product. in addition, the shipping is on time and we are delight that have selleck as our research parter.

  • Qingsong Liu, Ph.D
    Prof. Nathanael Gray Lab Dana-Farber Cancer Institute Biological Chemistry and Molecular Pharmacology Harvard Medical School

  •   
  • The AZD6244 works great.

  • Todd.Pitts
    ucdenver.edu

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;Oncogene, 2012, 31, 3277–3286


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;Nat Genet, 2011, 43(11), 1119-26.

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