Pexmetinib 是一种口服生物可利用的双重 p38 MAPK/Tie-2 抑制剂，可研究急性骨髓性白血病。在 HEK-293 细胞系中的 IC50 为 4 nM/18 nM。

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.

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 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]

945614-12-0

C31H33FN6O3

556.63

ARRY-614

H2O:<1 mgml
DMSO:93 mg/mL (167.1 mM)
Ethanol:93 mg/mL (167.1 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years