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HomeProduct name listPD184352

PD184352

Synonym(s):2-(2-Chloro-4-iodophenylamino)-N-cyclopropylmethoxy-3,4-difluorobenzamide;CI-1040

PD184352 Structural

What is PD184352?

Chemical properties

Off-White to Pale Beige Solid

The Uses of PD184352

An inhibitor of ERK signaling pathway. A MAP kinase inhibitor

The Uses of PD184352

An inhibitor of ERK signaling pathway. A MAP kinase inhibitor. Potent MEK inhibitor.

What are the applications of Application

PD 184,352 is a MEK inhibitor

Definition

ChEBI: 2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide is an aminobenzoic acid.

Biological Activity

pd184352 (also known as ci-1040), a benzhydroxamate derivative, is a potent and highly selective mek1/2, two members of the family of mapkks, inhibitor that inhibits purified mek1 with ic50 of 17 nm in a non-atp and non-erk1/2 competitive manner [1].pd184352 binds to a hydrophobic pocket, which is located in a region with low sequence homology to other kinases, adjacent to the mg-atp binding site of mek1 and mek2 inducing a conformational change in un-phosphorylated mek1/2 and hence inactivating the un-phosphorylated mek1/2 [1].pd184352 has been found to be actively against tumors, where it inhibits the growth of colon carcinomas in mouse xenograft models [1].

Biochem/physiol Actions

PD184352 (CI-1040) is a highly selective non-competitive inhibitor of MEK (MKK1; MAPK kinase) and the closely related MKK2. It has anti-cancer activity, suppresses the ERK pathway, and has been used along with other classes of inhibitors to establish embryonic stem cell lines.

storage

Store at +4°C

References

[1] frémin c, meloche s. from basic research to clinical development of mek1/2 inhibitors for cancer therapy. j hematol oncol. 2010 feb 11;3:8. doi: 10.1186/1756-8722-3-8.

Properties of PD184352

Melting point: 166-169°C
Density  1.747±0.06 g/cm3(Predicted)
storage temp.  room temp
solubility  DMSO: ≥30mg/mL
pka -5.58±0.50(Predicted)
form  powder
color  white to tan

Safety information for PD184352

Signal word Warning
Pictogram(s)
ghs
Environment
GHS09
GHS Hazard Statements H400:Hazardous to the aquatic environment, acute hazard
Precautionary Statement Codes P273:Avoid release to the environment.

Computed Descriptors for PD184352

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