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Pexmetinib

Catalog No. T6934 CAS 945614-12-0

Synonyms: ARRY-614

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.

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Pexmetinib, CAS 945614-12-0

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

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.
Targets&IC50	p38 MAPK:4 nM, Tie-2:18 nM
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]

Synonyms	ARRY-614
Molecular Weight	556.642
Formula	C31H33FN6O3
CAS No.	945614-12-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: <1 mg/mL

DMSO: 93 mg/mL (167.1 mM)

Ethanol: 93 mg/mL (167.1 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Koch K. 2013 AACR Annual Meeting.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Autophagy Compound Library Anti-Obesity Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library Immunology/Inflammation Compound Library Kinase Inhibitor Library MAPK Inhibitor Library Stem Cell Differentiation Compound Library Cytoskeletal Signaling Pathway Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Pexmetinib 945614-12-0 MAPK信号通路蛋白酪氨酸激酶自噬 Autophagy p38 MAPK Tie-2 ARRY 614 Inhibitor ARRY614 ARRY-614 inhibit inhibitor

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