Pexmetinib (ARRY-614)

For research use only.

Catalog No.S7799

3 publications

Pexmetinib (ARRY-614) Chemical Structure

CAS No. 945614-12-0

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.

Selleck's Pexmetinib (ARRY-614) has been cited by 3 publications

Purity & Quality Control

Choose Selective p38 MAPK Inhibitors

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.
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]

Methods Test Index PMID
Western blot
p-Tie2 / phospho-p38 ; 

PubMed: 27287719     

HEK-Tie2 cells express high basal levels of p-p38 and were induced to express constitutively active p-Tie-2 by 24 hr preincubation with doxycyclin. Following 2 hr treatment with varying concentrations of pexmetinib, samples were immunoblotted for p-Tie2 and p-p38 then normalized to GAPDH.

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]


Animal Research:


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  • Animal Models: Male Swiss Webster mice
  • 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


CAS No. 945614-12-0
Storage powder
in solvent
Synonyms N/A
Smiles CC1=CC=C(C=C1)N2C(=CC(=N2)C(C)(C)C)NC(=O)NCC3=C(C=CC(=C3)F)OC4=CC5=C(C=C4)N(N=C5)CCO

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p38 MAPK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID