444968

PD 0325901

≥95% (HPLC), liquid, MEK1/2 inhibitor, Calbiochem^®

• Synonym(s): InSolution MEK1/2 Inhibitor III, PD0325901, PD 0325901, N-((2R)-2,3-Dihyroxypropoxy)-3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)-benzamide, PD325901
• Empirical Formula (Hill Notation): C₁₆H₁₄F₃IN₂O₄
• CAS Number: 391210-10-9
• Molecular Weight: 482.19
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD08435926
• Assay: ≥95% (HPLC)
• Form: liquid
• Storage condition: OK to freeze, desiccated (hygroscopic), protect from light

Properties

• Product Name: MEK1/2 Inhibitor III, PD0325901, InSolution, ≥95%
• Quality Segment: 100
• assay: ≥95% (HPLC)
• form: liquid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, desiccated (hygroscopic), protect from light
• shipped in: ambient
• storage temp.: −20°C
• SMILES string: Ic1cc(c(cc1)Nc2c(c(ccc2C(=O)NOC[C@H](O)CO)F)F)F
• 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

PD-0325901 is a highly effective oral small-molecule inhibitor that targets both mitogen-activated protein kinase kinase 1 (MEK1) and MEK2. It is a selective, non-ATP-competitiveinhibitor of these two MEK isoforms. This cell-permeable benzamide compound is a selective non-competitive inhibitor of MAPKK/MKK, effectively blocking cellular Erk1/2 phosphorylation. In serum-starved HeLa cells, it achieves over 90% inhibition after serum stimulation, while in C26 cells, it reduces phosphorylation by 50% at inhibitor concentrations of 25 nM and 0.33 nM, respectively. The compound exhibits minimal to no effect on Erk1/2 activity ora panel of 66 other kinases, even at concentrations as high as 10 µM in cell-free kinase assays. PD-0325901 has demonstrated oral bioavailability inmice, successfully suppressing both tumor growth and Erk phosphorylation in BRAF(V600E)-expressing SKMEL28 cell-derived tumors in vivo.

Application

PD 0325901 has been used as:·

• a supplement in induced pluripotent stem cells (iPSC) medium to culture MEF feeder layers with reprogrammed cells
• mitogen-activated protein kinase kinase1/2 (MEK1/2) inhibitor to treat the cells to identify G1 phase cells that had crossed the restriction point in the cell cycle
• Mek1/2 inhibitor to block the Ras-Erk1/2 signaling pathwayto investigate the role of fibroblast growth factor (Fgf) signaling in the specification of endoderm progenitors during embryonic development

Packaging

Packaged under inert gas

Physical form

A 50 mM (5 mg/207 µl) solution of MEK1/2 Inhibitor III, PD0325901 (Cat. No. 444966 ) in DMSO.

Legal Information

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

Disclaimer

Toxicity: Regulatory Review (Z)

Safety Information

• Storage Class: 10 - Combustible liquids
• WGK: WGK 2
• Flash Point (°F): 188.6 °F - closed cup - (refers to pure substance)
• Flash Point (°C): 87 °C - closed cup - (refers to pure substance)