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444966 MEK1/2 Inhibitor III - CAS 391210-10-9 - Calbiochem

MEK1/2 Inhibitor III, CAS 391210-10-9, is a cell-permeable, non-competitive, highly potent MEK/MAPKK/MKK inhibitor that blocks cellular Erk1/2 phosphorylation (IC50 = 25 in serum starved HeLa cells).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N-((2R)-2,3-Dihyroxypropoxy)-3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)-benzamide, PD 0325901, PD325901, PD0325901, MEK Inhibitor III

444966
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
391210-10-9C₁₆H₁₄F₃IN₂O₄

Products

Catalogue NumberPackaging Qty/Pack
444966-5MG Plastic ampoule 5 mg
Description
OverviewA cell-permeable benzamide compound that acts as a non-competitive, highly potent, selective MEK/MAPKK/MKK inhibitor and effectively blocks cellular Erk1/2 phosphorylation (by >90% in serum-starved HeLa after serum-stimulation and 50% in C26 with 25 and 0.33 nM inhibitor, respectively), while exhibiting little or no effect against the activity of Erk1/2 or a panel of 66 other kinases even at concentrations as high as 10 µM in cell-free kinase assays. Shown to be orally available in mice and suppress both the growth of and Erk phosphorylation in BRAF(V600E)-expressing SKMEL28 cell-derived tumor in vivo. Also available in InSolution™ format (Cat. No. 444968).
Catalogue Number444966
Brand Family Calbiochem®
SynonymsN-((2R)-2,3-Dihyroxypropoxy)-3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)-benzamide, PD 0325901, PD325901, PD0325901, MEK Inhibitor III
References
ReferencesBarrett, S.D., et al. 2008. Bioorg. Med. Chem. Lett. 18, 6501.
Leyton, J., et al. 2008. Mol. Cancer Ther. 7, 3112.
Silva, J., et al. 2008. PLoS Biol. 6, 2237.
Ying, Q.L., et al. 2008. Nature 453, 519.
Bain, J., et al. 2007. Biochem. J. 408, 297.
Solit, D.B., et al. 2006. Nature 439, 358.
Product Information
CAS number391210-10-9
FormWhite to off-white solid
Hill FormulaC₁₆H₁₄F₃IN₂O₄
Chemical formulaC₁₆H₁₄F₃IN₂O₄
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
ApplicationMEK1/2 Inhibitor III, CAS 391210-10-9, is a cell-permeable, non-competitive, highly potent MEK/MAPKK/MKK inhibitor that blocks cellular Erk1/2 phosphorylation (IC50 = 25 in serum starved HeLa cells).
Biological Information
Purity≥95% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
444966-5MG 04055977204520

Documentation

MEK1/2 Inhibitor III - CAS 391210-10-9 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

MEK1/2 Inhibitor III - CAS 391210-10-9 - Calbiochem Certificates of Analysis

TitleLot Number
444966

References

Reference overview
Barrett, S.D., et al. 2008. Bioorg. Med. Chem. Lett. 18, 6501.
Leyton, J., et al. 2008. Mol. Cancer Ther. 7, 3112.
Silva, J., et al. 2008. PLoS Biol. 6, 2237.
Ying, Q.L., et al. 2008. Nature 453, 519.
Bain, J., et al. 2007. Biochem. J. 408, 297.
Solit, D.B., et al. 2006. Nature 439, 358.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision07-May-2018 JSW
SynonymsN-((2R)-2,3-Dihyroxypropoxy)-3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)-benzamide, PD 0325901, PD325901, PD0325901, MEK Inhibitor III
DescriptionA cell-permeable benzamide compound that acts as a non-competitive, highly potent, selective MEK/MAPKK/MKK inhibitor and effectively blocks cellular Erk1/2 phosphorylation (by >90% in serum-starved HeLa after serum-stimulation and 50% in C26 with 25 and 0.33 nM inhibitor, respectively), while exhibiting little or no effect against the activity of Erk1/2 or a panel of 66 other kinases even at concentrations as high as 10 µM in cell-free kinase assays. Shown to be orally available in mice and suppress both the growth of and Erk phosphorylation in BRAF(V600E)-expressing SKMEL28 cell-derived tumor in vivo.
FormWhite to off-white solid
Intert gas (Yes/No) Packaged under inert gas
CAS number391210-10-9
Chemical formulaC₁₆H₁₄F₃IN₂O₄
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (20 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesBarrett, S.D., et al. 2008. Bioorg. Med. Chem. Lett. 18, 6501.
Leyton, J., et al. 2008. Mol. Cancer Ther. 7, 3112.
Silva, J., et al. 2008. PLoS Biol. 6, 2237.
Ying, Q.L., et al. 2008. Nature 453, 519.
Bain, J., et al. 2007. Biochem. J. 408, 297.
Solit, D.B., et al. 2006. Nature 439, 358.