[CAS NO. 945614-12-0] Pexmetinib (ARRY-614)

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PRODUCTS SPECIFICATIONS [945614-12-0]

Catalog

SLK-S7799

Brand

Selleck

CAS

945614-12-0

DESCRIPTION [945614-12-0]

Overview

MDL	MFCD28502055
Molecular Weight	556.63
Molecular Formula	C31H33FN6O3
SMILES	O=C(NCC1=CC(F)=CC=C1OC2=CC3=C(N(CCO)N=C3)C=C2)NC4=CC(C(C)(C)C)=NN4C5=CC=C(C)C=C5

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Description

Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual inhibitor with 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.

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.

References

[1] Koch K. 2013 AACR Annual Meeting.