Pexmetinib (ARRY-614)

Catalog No.S7799

Pexmetinib (ARRY-614) Chemical Structure

Molecular Weight(MW): 556.63

Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.

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Biological Activity

Description Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.
Targets
p38 MAPK [1] Tie-2 [1]
In vitro

In HeLa cells, Pexmetinib inhibits phospho-HSP27 with IC50 of 2 nM. In isolated PBMCs and human whole blood cells, Pexmetinib inhibits LPS-Induced TNFα with IC50 of 4.5 nM and 313 nM, respectively. [1]

In vivo In male Swiss Webster mice, Pexmetinib (30 mg/kg, p.o.) inhibits the production of the proinfl ammatory cytokines TNFα and IL6 in response to lipopolysaccharide (LPS) or staphyloccus enterotoxin A. In established RPMI 8226 xenografts, ARRY-614 (25 mg/kg, p.o.) inhibits tumor growth and shows additive activity when combines with thalidomide. In ovarian carcinoma A2780 xenografts, ARRY-614 (30 mg/kg, p.o.) also shows additive tumor growth inhibition activity when combines with Taxol. [1]

Protocol

Animal Research:

[1]

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  • Animal Models: Male Swiss Webster mice
  • Formulation: --
  • Dosages: 30 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (179.65 mM)
Ethanol 100 mg/mL (179.65 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 556.63
Formula

C31H33FN6O3

CAS No. 945614-12-0
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01496495 Completed Myelodysplastic Syndromes Array BioPharma January 2012 Phase 1
NCT00916227 Completed Myelodysplastic Syndromes Array BioPharma June 2009 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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p38 MAPK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID