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Merck

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

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About This Item

Empirical Formula (Hill Notation):
C16H14F3IN2O4
CAS Number:
391210-10-9
Molecular Weight:
482.19
MDL number:
MFCD08435926
UNSPSC Code:
12352200
NACRES:
NA.77

Product Name

MEK1/2 Inhibitor III, PD0325901, InSolution, ≥95%

Quality Level

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

Related Categories

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)

Storage Class Code

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)

Certificates of Analysis (COA)

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Scott G Wilcockson et al.
Developmental cell, 58(23), 2802-2818 (2023-09-16)
Extracellular signal-regulated kinase (Erk) signaling dynamics elicit distinct cellular responses in a variety of contexts. The early zebrafish embryo is an ideal model to explore the role of Erk signaling dynamics in vivo, as a gradient of activated diphosphorylated Erk (P-Erk)
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Developmental cell, 57(23), 2604-2622 (2022-12-07)
Specification of the germ layers by Nodal signaling has long been regarded as an archetype of how graded morphogens induce different cell fates. However, this deterministic model cannot explain why only a subset of cells at the early zebrafish embryo
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