SelumetinibA MEK-1 non-ATP competitive inhibitor

Selumetinib (CAS 606143-52-6)

Selumetinib | CAS 606143-52-6 is rated 5.0 out of 5 by 1.
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Synonym: AZD6244
Application: A MEK-1 non-ATP competitive inhibitor
CAS Number: 606143-52-6
Purity: ≥98%
Molecular Weight: 457.68
Molecular Formula: C17H15BrClFN4O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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Selumetinib is a non-ATP competitive inhibitor of MEK-1 (IC50 = 14 nM). This compound inactivates the phosphorylation of ERK1/2 (IC50 < 40 nM). Selumetinib has little effect on p38, c-Jun-NH2-kinase, or the MEK/ERK5 pathways.

Appearance :
Crystalline granules or crystalline powder
Physical State :
Solid
Solubility :
Soluble in DMSO (92 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (<1 mg/ml at 25 °C).
Storage :
Store at -20° C
Melting Point :
208-214° C
Boiling Point :
644.98° C (Predicted)
Density :
~1.7 g/cm3 (Predicted)
Refractive Index :
n20D 1.67 (Predicted)
IC50 :
CHP-212: IC50 = 3.15 nM (human); MEK1: IC50 = 14 nM; H9: IC50 = 22.88 nM (human); MEK2: IC50 = 530 nM; EGF receptor: IC50 = 7.0 µM
pK Values :
pKb: 2.92 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
10127622
MDL Number :
MFCD11977472
SMILES :
CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)Cl)C(=O)NOCCO

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Certificate of Analysis

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Selumetinib  Product Citations

See how others have used Selumetinib. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 28383550  Wassermann-Dozorets, R. et al. 2017. Cell Death Dis. 8: e2733.

Citations 1 to 1 of 1 total
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Rated 5 out of 5 by from Dreaden Dreaden, EC. et al. (PubMed 26034127) co-encapsulated AZD6244 (Selumetinib), an inhibitor of Mek1/2, and PX-866 (sc-396764), an inhibitor of PI3K, to create tumor-targeting nanoscale drug formulation-layer-by-layer (LbL) nanoparticles. Combined MAPK and PI3K axis blockade from the nanoscale formulations was synergistically toxic toward triple-negative breast (MDA-MB-231) and RAS-mutant lung tumor cells (KP7B) in vitro. -SCBT Publication Review
Date published: 2015-01-31
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