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文件

PZ0162

Sigma-Aldrich

PD 0325901

≥98% (HPLC)

别名:

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

经验公式（希尔记法）:
C16H14F3IN2O4
CAS号:
391210-10-9
分子量:
482.19
MDL编号:
MFCD08435926
UNSPSC代码:
12352200
PubChem化学物质编号:
329823743

质量水平

100

检测方案

≥98% (HPLC)

形式

powder

旋光性

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

颜色

white to off-white

溶解性

DMSO: 20 mg/mL, clear

储存温度

2-8°C

SMILES字符串

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 key

SUDAHWBOROXANE-SECBINFHSA-N

基因信息

human ... MAP2K1(5604) , MAP2K2(5605)

应用

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。

特点和优势

《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。

其他说明

2024年CiteAb奖——成功的帕金森研究供应商(2024 CiteAb Award Winner for Supplier Succeeding in Parkinson′s Research)

象形图

Skull and crossbonesHealth hazard
GHS06,GHS08

警示用语：

Danger

危险声明

H301,H373,H413

危险分类

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

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

分析证书(COA)

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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)
Bin Zhang et al.
The Journal of clinical investigation, 126(3), 975-991 (2016-02-16)
Chronic myelogenous leukemia (CML) results from transformation of a long-term hematopoietic stem cell (LTHSC) by expression of the BCR-ABL fusion gene. However, BCR-ABL-expressing LTHSCs are heterogeneous in their capacity as leukemic stem cells (LSCs). Although discrepancies in proliferative, self-renewal, and
Inhibition of glioblastoma dispersal by the MEK inhibitor PD0325901
Shannon S, et al.
BMC Cancer, 17(1), 121-121 (2017)
Feeder-Free Derivation of Naive Human Pluripotent Stem Cells
Ward E, et al.
Stem Cells and Development, 26(15), 1087-1089 (2017)
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
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