444966

MEK1/2 Inhibitor III

The MEK1/2 Inhibitor III, also referenced under CAS 391210-10-9, controls the biological activity of MEK1/2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): MEK1/2 Inhibitor III, PD325901, PD0325901, N-((2R)-2,3-Dihyroxypropoxy)-3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)-benzamide, PD 0325901, MEK Inhibitor III
• Empirical Formula (Hill Notation): C₁₆H₁₄F₃IN₂O₄
• CAS Number: 391210-10-9
• Molecular Weight: 482.19
• MDL number: MFCD08435926
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white to off-white
• solubility: DMSO: 20 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C16H14F3IN2O4/c17-11-3-2-10(16(25)22-26-7-9(24)6-23)15(14(11)19)21-13-4-1-8(20)5-12(13)18/h1-5,9,21,23-24H,6-7H2,(H,22,25)/t9-/m1/s1
• InChI key: SUDAHWBOROXANE-SECBINFHSA-N

Description

General description

A 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.

A 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).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

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. Nature453, 519.
Bain, J., et al. 2007. Biochem. J.408, 297.
Solit, D.B., et al. 2006. Nature439, 358.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Pictograms: GHS06,GHS08
• Signal Word: Danger
• Hazard Statements: H301,H373,H413
• Precautionary Statements: P260 - P264 - P273 - P301 + P310 - P314 - P405
• Hazard Classifications: Acute Tox. 3 Oral - Aquatic Chronic 4 - STOT RE 2
• Storage Class Code: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable