945614-12-0

945614-12-0 structure

Name: Pexmetinib
Chemical Name: 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[[5-fluoro-2-[1-(2-hydroxyethyl)indazol-5-yl]oxyphenyl]methyl]urea
CAS Number: 945614-12-0
Molecular Formula: C₃₁H₃₃FN₆O₃
Molecular Weight: 556.630
Catalog: Signaling Pathways MAPK/ERK Pathway p38 MAPK
Create Date: 2016-12-06 06:43:50
Modify Date: 2024-01-08 17:18:40
Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.

Name	1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[[5-fluoro-2-[1-(2-hydroxyethyl)indazol-5-yl]oxyphenyl]methyl]urea
Synonyms	ARRY-614 pexmétinib pexmetinib 1-(5-Fluoro-2-{[1-(2-hydroxyethyl)-1H-indazol-5-yl]oxy}benzyl)-3-[1-(4-methylphenyl)-3-(2-methyl-2-propanyl)-1H-pyrazol-5-yl]urea Urea, N-[3-(1,1-dimethylethyl)-1-(4-methylphenyl)-1H-pyrazol-5-yl]-N'-[[5-fluoro-2-[[1-(2-hydroxyethyl)-1H-indazol-5-yl]oxy]phenyl]methyl]- UNII-3750D0U8B5

Description	Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.
Related Catalog	Signaling Pathways >> MAPK/ERK Pathway >> p38 MAPK Research Areas >> Cancer
Target	IC50: 1 nM (Tie-2), 35 nM (p38α), 26 nM (p38β)[1]
In Vitro	Pexmetinib is a Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively. Pexmetinib also shows IC50s of 4 nM (Abl), 10 nM (Arg), 28 nM (FGFR1), 47 nM (Flt1), 42 nM (Flt4), 41 nM (Fyn), 26 nM (Hck), 25 nM (Lyn), and 26 nM (MINK), respectively. Pexmetinib (0.5, 1 μM) blocks leukemic cell proliferation and stimulates hematopoietic activity in myelodysplastic syndromes[1].
Cell Assay	Cell lines and primary samples are incubated at indicated doses of of TIE2/p38 inhibitor Pexmetinib. Viability is assessed by addition of Cell Titer Blue and measured via Fluostar Omega Microplate reader[1].
References	[1]. Bachegowda L, et al. Pexmetinib: A Novel Dual Inhibitor of Tie2 and p38 MAPK with Efficacy in Preclinical Models of Myelodysplastic Syndromes and Acute Myeloid Leukemia. Cancer Res. 2016 Aug 15;76(16):4841-4849.