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XL-784

Catalog No. T13358Cas No. 1224964-36-6

XL-784 is a selective inhibitor of matrix metalloproteinases (MMP)(IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1,MMP-2,MMP-3,MMP-8,MMP-9,MMP-13,respectively).

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Pack Size	Price	Availability
2 mg	$198	5 days
5 mg	$332	5 days
25 mg	$987	8-10 weeks
50 mg	$1,360	8-10 weeks
100 mg	$1,990	8-10 weeks

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Product Introduction

Bioactivity

Description	XL-784 is a selective inhibitor of matrix metalloproteinases (MMP)(IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1,MMP-2,MMP-3,MMP-8,MMP-9,MMP-13,respectively).
In vitro	XL-784 is a low-molecular-weight (1,122 g/mol) MMPs inhibitor. XL-784 potently inhibits MMP-2, MMP-13, and ADAM10 [TNF-α-converting enzyme (TACE)] activity in vitro(IC50 values in the range of 1-2 nM). XL-784 also inhibits MMP-9 (IC50 ~20 nM) activity and ADAM17 (IC50 ~70 nM) also known as TACE. However, XL-784 exhibits low potency for inhibition of MMP-1 (IC50 ~2,000 nM)[1].
In vivo	Treatment with all doses of XL-784 and doxycycline are effective in inhibiting aortic dilatation. There is a clear dose-response relationship between XL-784 and reductions in aortic dilatation at harvest (50 mg/kg 140.4% ±3.2%; 125 mg/kg 129.3% ±5.1%; 250 mg/kg 119.2%±3.5%; all Ps<0.01 compared to control). This continues with the higher doses (375 mg/kg 88.6%±4.4%; 500 mg/kg 76.0%±3.5%). he two doses of the highest dose of XL-784 tested were more effective than doxycycline in inhibiting the maximum expansion of the aorta after elastase infusion (112.2%±2.0%, P<0.05) [2].

Chemical Properties

Molecular Weight	1126.17
Formula	C42H46Cl2F4MgN6O16S2
Cas No.	1224964-36-6

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 110 mg/mL (200.03 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	0.8880 mL	4.4398 mL	8.8797 mL	44.3983 mL
5 mM	0.1776 mL	0.8880 mL	1.7759 mL	8.8797 mL
10 mM	0.0888 mL	0.4440 mL	0.8880 mL	4.4398 mL
20 mM	0.0444 mL	0.2220 mL	0.4440 mL	2.2199 mL
50 mM	0.0178 mL	0.0888 mL	0.1776 mL	0.8880 mL
100 mM	0.0089 mL	0.0444 mL	0.0888 mL	0.4440 mL

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In Vivo Formulation Calculator (Clear solution)

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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

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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

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Tech Support

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