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Merck
CN

444968

PD 0325901

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

别名:

InSolution MEK1/2 抑制剂III, PD0325901, PD 0325901,N-((2R)-2,3-二羟丙氧基)-3,4-二氟-2-((2-氟-4-碘苯基)氨基)-苯甲酰胺,PD325901

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关于此项目

经验公式(希尔记法):
C16H14F3IN2O4
化学文摘社编号:
分子量:
482.19
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥95% (HPLC)
Form:
liquid
Quality level:
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
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产品名称

MEK1/2抑制剂III,PD0325901, InSolution, ≥95%

Quality Level

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

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

用惰性气体包装

Physical form

50 mM(5 mg/207 µl)MEK1/2抑制剂III,PD0325901(目录号444966)的DMSO溶液。

Legal Information

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

Disclaimer

毒性:监管审查(Z)


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存储类别

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)



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全球贸易项目编号

货号GTIN
444968-5MG04055977204544