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Pexmetinib

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Purity:99.66%

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COA HPLC HNMR

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 Size	Price	Availability
2 mg	$54	In Stock
5 mg	$98	In Stock
10 mg	$157	In Stock
25 mg	$316	In Stock
50 mg	$539	In Stock
100 mg	$597	In Stock
1 mL x 10 mM (in DMSO)	$121	In 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]
Alias	ARRY-614

Chemical Properties

Molecular Weight	556.63
Formula	C31H33FN6O3
Cas No.	945614-12-0

Storage & Solubility Information

Storage

Powder: -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

	1mg	5mg	10mg	50mg
1 mM	1.7965 mL	8.9826 mL	17.9653 mL	89.8263 mL
5 mM	0.3593 mL	1.7965 mL	3.5931 mL	17.9653 mL
10 mM	0.1797 mL	0.8983 mL	1.7965 mL	8.9826 mL
20 mM	0.0898 mL	0.4491 mL	0.8983 mL	4.4913 mL
50 mM	0.0359 mL	0.1797 mL	0.3593 mL	1.7965 mL
100 mM	0.0180 mL	0.0898 mL	0.1797 mL	0.8983 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

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Tech Support

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