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
产品名称
MEK1/2抑制剂III，PD0325901, InSolution, ≥95%
质量水平
方案
≥95% (HPLC)
表单
liquid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
desiccated (hygroscopic)
protect from light
运输
ambient
储存温度
−20°C
SMILES字符串
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
一般描述
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.
应用
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
包装
用惰性气体包装
外形
50 mM（5 mg/207 µl）MEK1/2抑制剂III，PD0325901（目录号444966）的DMSO溶液。
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
毒性：监管审查（Z）
储存分类代码
10 - Combustible liquids
WGK
WGK 2
闪点(°F)
188.6 °F - closed cup - (refers to pure substance)
闪点(°C)
87 °C - closed cup - (refers to pure substance)
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