PD318088 - 10mM in DMSO , CAS No.391210-00-7

CAS: 391210-00-7 Cat. No.: P408043 Fórmula: C₁₆H₁₃BrF₃IN₂O₄ Peso molecular: 561.1

CALIDAD & PUREZA 10mM in DMSO

Synonyms

5-bromo-N-(2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodophenylamino)benzamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

PD318088 is a non-ATP competitive allostericMEK1/2inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.
In vitro

PD318088 is a small-molecule inhibitor of MEK1/2, which is an analog of PD184352, suggesting it might have substantial anti-proliferative activity against cancer cells, although no functional study of PD318088 is currently available. PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. Formation of the ternary complexes with PD318088 and MgATP results in moderate increases (to 140 nM) for the K_d monomer-dimer for both MEK1 and MEK2. The binding of PD318088 and MgATP to MEK1 also abolishes the formation of tetramers and higher-order aggregates. PD318088 and MgATP together increase the dimerization disassociation constant for MEK1 and MEK2 slightly from ~75 nM to ~140 nM, suggesting that the mechanism of inhibition for PD318088 is probably a result of localized conformational changes in the active site and not a global change in the overall structure.

In vivo

Cell Data

cell lines：HUVEC

Concentrations：

Incubation Time：

Powder Purity:≥99%

Especificaciones

Sinónimos

5-bromo-N-(2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodophenylamino)benzamide

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Nombres e identificadores

Isómeros SMILES

C1=CC(=C(C=C1I)F)NC2=C(C(=C(C=C2C(=O)NOCC(CO)O)Br)F)F

Peso molecular

561.1

Reaxy-Rn

13493289

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=13493289&ln=

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 48 mg/mL (196.51 mM); Ethanol: 48 mg/mL (196.51 mM); Water: Insoluble