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Pexmetinib

Pexmetinib
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Purity:99.66%
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Pexmetinib

Catalog No. T6934Cas No. 945614-12-0
Pexmetinib (ARRY-614) (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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Pack SizePrice/USDAvailabilityQuantity
2 mg$54In Stock
5 mg$98In Stock
10 mg$157In Stock
25 mg$316In Stock
50 mg$539In Stock
100 mg$597In Stock
1 mL x 10 mM (in DMSO)$121In Stock
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Product Introduction

Bioactivity
Description
Pexmetinib (ARRY-614) (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.
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 proin? 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]
AliasARRY-614
Chemical Properties
Molecular Weight556.63
FormulaC31H33FN6O3
Cas No.945614-12-0
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 93 mg/mL (167.1 mM)
Ethanol: 93 mg/mL (167.1 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.7965 mL8.9826 mL17.9653 mL89.8263 mL
5 mM0.3593 mL1.7965 mL3.5931 mL17.9653 mL
10 mM0.1797 mL0.8983 mL1.7965 mL8.9826 mL
20 mM0.0898 mL0.4491 mL0.8983 mL4.4913 mL
50 mM0.0359 mL0.1797 mL0.3593 mL1.7965 mL
100 mM0.0180 mL0.0898 mL0.1797 mL0.8983 mL

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