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PZ0162

PD 0325901

≥98% (HPLC), MKK1 (MEK1) and MKK2 (MEK2) inhibitor, powder

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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关于此项目

经验公式（希尔记法）:
C16H14F3IN2O4
化学文摘社编号:
391210-10-9
分子量:
482.19
PubChem Substance ID:
329823743
UNSPSC Code:
12352200
MDL number:
MFCD08435926
NACRES:
NA.28
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100
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产品名称

PD 0325901, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

powder

optical activity

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

color

white to off-white

solubility

DMSO: 20 mg/mL, clear

storage temp.

2-8°C

SMILES string

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

Gene Information

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

Application

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。

Biochem/physiol Actions

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。
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％。
PD 0325901是一种有效的MKK1（MEK1）和MKK2（MEK2）抑制剂。

Features and Benefits

《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。

Other Notes

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)

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pictograms

Skull and crossbonesHealth hazard
GHS06,GHS08

signalword

Danger

Hazard Classifications

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

存储类别

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

flash_point_f

Not applicable

flash_point_c

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000338680
0000243126
0000338680
0000243126
0000212164

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商品

MAPKKKs

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 Cell Culture in Serum-Free Media

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

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)
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
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