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Merck

PZ0162

PD 0325901

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

Synonyme(s) :

N-[(2R)-2,3-Dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-benzamide

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A propos de cet article

Formule empirique (notation de Hill) :
C16H14F3IN2O4
Numéro CAS:
Poids moléculaire :
482.19
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
NACRES:
NA.28
Assay:
≥98% (HPLC)
Form:
powder
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Nom du produit

PD 0325901, ≥98% (HPLC)

Quality Segment

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

Application

PD 0325901 has been used as an inhibitor in extracellular signal-regulated kinase (ERK) inhibition assay in primed induced pluripotent stem cells, RKO colorectal cancer cell line and human embryonic stem cells(hESCs).

Biochem/physiol Actions

PD 0325901 is a potent MKK1 (MEK1) and MKK2 (MEK2) inhibitor.
PD 0325901 is a potent MKK1 (MEK1) and MKK2 (MEK2) inhibitor. The Ki is 1.1 and 0.79 nM for MEK1 and MEK2, respectively. PD 0325901 was inactive against a panel of 27 other kinases. PD 0325901 inhibited C26 tumor pERK by 75% when dosed at 25 mg/kg in mice.
PD 0325901 by inhibiting mitogen-activated protein kinases (MAPKs) elicits growth-inhibitory and antiangiogenic effects on glioblastoma and melanoma tumor progression.

Features and Benefits

This compound is featured on the MAPKKKs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.


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pictograms

Skull and crossbonesHealth hazard

signalword

Danger

Hazard Classifications

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

Classe de stockage

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



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