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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
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD08435926
Assay:
≥95% (HPLC)
Form:
liquid
Quality level:
100
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light

Key Documents

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Product Name

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

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

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

Quality Level

100

Related Categories

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

Disclaimer

Toxicity: Regulatory Review (Z)

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.

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

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)

Regulatory Listings

Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.

Group 4: Flammable liquids + Type 3 petroleums + Hazardous rank III + Water insoluble liquid

fsl

Substances Subject to be Indicated Names

ishl_indicated

Substances Subject to be Notified Names

ishl_notified

444968-5MG:

jan

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Zhao Yang et al.
Journal of biochemical and molecular toxicology, 36(12), e23219-e23219 (2022-09-20)
Polyphyllin I (PPI) is a famous traditional medicine ingredient, which has been explored in wide range of areas. Nevertheless, whether PPI exerts any functions in coronary artery disease (CAD) is still uncertified. Herein, we probed the effect and mechanism of
Gayan I Balasooriya et al.
Nature communications, 13(1), 5984-5984 (2022-10-11)
Each mammalian autosomal gene is represented by two alleles in diploid cells. To our knowledge, no insights have been made in regard to allele-specific regulatory mechanisms of autosomes. Here we use allele-specific single cell transcriptomic analysis to elucidate the establishment
Shihai Zhang et al.
PLoS genetics, 17(10), e1009832-e1009832 (2021-10-22)
The mammalian target of rapamycin complex 1 (mTORC1) senses multiple stimuli to regulate anabolic and catabolic processes. mTORC1 is typically hyperactivated in multiple human diseases such as cancer and type 2 diabetes. Extensive research has focused on signaling pathways that
Jenny F Nathans et al.
Science advances, 7(3) (2021-02-02)
The G1-S checkpoint is thought to prevent cells with damaged DNA from entering S phase and replicating their DNA and efficiently arrests cells at the G1-S transition. Here, using time-lapse imaging and single-cell tracking, we instead find that DNA damage
Aurélia Huyghe et al.
Nature cell biology, 22(4), 389-400 (2020-04-02)
In mouse embryonic stem cells (mESCs), chemical blockade of Gsk3α/β and Mek1/2 (2i) instructs a self-renewing ground state whose endogenous inducers are unknown. Here we show that the axon guidance cue Netrin-1 promotes naive pluripotency by triggering profound signalling, transcriptomic

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Global Trade Item Number

SKUGTIN
444968-5MGCN04055977204544

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