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444966

PD 0325901

≥95% (HPLC), MEK/MAPKK/MKK inhibitor, solid

Synonyme(s) :

MEK1/2 Inhibitor III, PD325901, PD0325901, N-((2R)-2,3-Dihyroxypropoxy)-3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)-benzamide, PD 0325901, MEK Inhibitor III

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A propos de cet article

Formule empirique (notation de Hill) :
C16H14F3IN2O4
Numéro CAS:
391210-10-9
Poids moléculaire :
482.19
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD08435926
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze, protect from light
Service technique
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Nom du produit

MEK1/2 Inhibitor III, The MEK1/2 Inhibitor III, also referenced under CAS 391210-10-9, controls the biological activity of MEK1/2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Quality Level

100

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

white to off-white

solubility

DMSO: 20 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

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

General description

A cell-permeable benzamide compound that acts as a non-competitive, highly potent, selective MEK/MAPKK/MKK inhibitor and effectively blocks cellular Erk1/2 phosphorylation (by >90% in serum-starved HeLa after serum-stimulation and 50% in C26 with 25 and 0.33 nM inhibitor, respectively), while exhibiting little or no effect against the activity of Erk1/2 or a panel of 66 other kinases even at concentrations as high as 10 µM in cell-free kinase assays. Shown to be orally available in mice and suppress both the growth of and Erk phosphorylation in BRAF(V600E)-expressing SKMEL28 cell-derived tumor in vivo. Also available in InSolution format (Cat. No. 444968).

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Barrett, S.D., et al. 2008. Bioorg. Med. Chem. Lett.18, 6501.
Leyton, J., et al. 2008. Mol. Cancer Ther.7, 3112.
Silva, J., et al. 2008. PLoS Biol.6, 2237.
Ying, Q.L., et al. 2008. Nature453, 519.
Bain, J., et al. 2007. Biochem. J.408, 297.
Solit, D.B., et al. 2006. Nature439, 358.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

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flash_point_c

Not applicable

pictograms

Skull and crossbonesHealth hazard
GHS06,GHS08

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

wgk

WGK 3

flash_point_f

Not applicable

Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

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