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PZ0162

Sigma-Aldrich

PD 0325901

≥98% (HPLC)

同義詞:

N-[(2R)-2,3-二羟基丙氧基]-3,4-二氟-2-[(2-氟-4-碘苯)氨基]苯甲酰胺

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About This Item

經驗公式(希爾表示法):
C16H14F3IN2O4
CAS號碼:
分子量::
482.19
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:

化驗

≥98% (HPLC)

形狀

powder

光學活性

[α]/D -1.8 to -3.5°, c = 1 mg/mL in methanol

顏色

white to off-white

溶解度

DMSO: 20 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

FC1=C(NC2=CC=C(I)C=C2F)C(C(NOC[C@H](O)CO)=O)=CC=C1F

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 密鑰

SUDAHWBOROXANE-SECBINFHSA-N

基因資訊

應用

PD 0325901作为抑制剂,用于细胞外信号调节激酶(ERK)抑制试验,在引物诱导性多能干细胞、 RKO结直肠癌细胞系 和人胚胎干细胞(hESCs)中进行。

生化/生理作用

PD 0325901是一种有效的MKK1(MEK1)和MKK2(MEK2)抑制剂。PD 0325901对MEK1和MEK2的Ki分别为1.1和0.79nM。PD 0325901对一组27种其他激酶无活性。以25mg/kg对小鼠给药时,PD 0325901对C26肿瘤pERK的抑制率达到75%。
通过抑制丝裂原激活的蛋白激酶(MAPK),PD 0325901对胶质母细胞瘤 和黑色素瘤的肿瘤进展产生抑制生长和抗血管生成作用。

特點和優勢

《受体分类和信号转导》手册的 MAPKKK 页面有该化合物的介绍。想要浏览手册的其他页面, 请单击此处

象形圖

Skull and crossbonesHealth hazard

訊號詞

Danger

危險聲明

危險分類

Acute Tox. 3 Oral - Aquatic Chronic 4 - STOT RE 2

儲存類別代碼

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


分析證明 (COA)

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存取文件庫

Madeleine Linneberg-Agerholm et al.
Development (Cambridge, England), 146(24) (2019-11-20)
Embryonic stem cells (ESCs) exist in at least two states that transcriptionally resemble different stages of embryonic development. Naïve ESCs resemble peri-implantation stages and primed ESCs the pre-gastrulation epiblast. In mouse, primed ESCs give rise to definitive endoderm in response
Feeder-Free Derivation of Naive Human Pluripotent Stem Cells
Ward E, et al.
Stem Cells and Development, 26(15), 1087-1089 (2017)
Growth-inhibitory and antiangiogenic activity of the MEK inhibitor PD0325901 in malignant melanoma with or without BRAF mutations
Ciuffreda L, et al.
Neoplasia, 11(8), 720-W6-720-W6 (2009)
Inhibition of glioblastoma dispersal by the MEK inhibitor PD0325901
Shannon S, et al.
BMC Cancer, 17(1), 121-121 (2017)
The role of autophagy in the treatment of BRAF mutant colorectal carcinomas differs based on microsatellite instability status
Koustas E, et al.
PLoS ONE, 13(11), e0207227-e0207227 (2018)

文章

The extracellular signal regulated kinase (ERK1 and ERK2) pathways are activated by mitogens and play an important role in controlling cell growth and differentiation.

Naive pluripotent stem cells cultured in vitro using specialized media and inhibitors mimic "ground-state" cells from blastocysts.

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