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IN-1130

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Purity:98.08%

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COA HPLC HNMR

IN-1130

Catalog No. T15572Cas No. 868612-83-3

IN-1130 is a selective inhibitor of ALK5 with IC50 values of 5.3 nM, 36 nM, and 4.3 μM for phosphorylation of ALK5-mediated Smad3, ALK5 phosphorylation of casein and p38α mitogen-activated protein kinase.

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Pack Size	Price	Availability
5 mg	$48	In Stock
10 mg	$83	In Stock
25 mg	$173	In Stock
50 mg	$273	In Stock
100 mg	$395	In Stock
1 mL x 10 mM (in DMSO)	$53	In Stock

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Product Introduction

Bioactivity

Description	IN-1130 is a selective inhibitor of ALK5 with IC50 values of 5.3 nM, 36 nM, and 4.3 μM for phosphorylation of ALK5-mediated Smad3, ALK5 phosphorylation of casein and p38α mitogen-activated protein kinase.
In vitro	IN-1130 (0.5 -1 μM) inhibits the phosphorylation and nuclear translocation of TGF-β-stimulated Smad2 in HepG2 and 4T1 cells. In MCF10A cells, IN-1130 (1 μM) restores the TGF-β-mediated decrease in E-cadherin protein expression, inhibits TGF-β-induced MMPs mRNA expression, and reduces the gelatinolytic activity of secreted MMPs[2].
In vivo	In unilateral ureteral obstruction rats, intraperitoneal administration of IN-1130 (10-20 mg/kg) decreases the extent of interstitial nephritis and fibrosis. dose-dependently reduces the levels of TGF-β1 mRNA and suppresses Smad2, α-SMA, myofibroblasts phosphorylation[1]. In MMTV/c-Neu mice intraperitoneal administration of IN-1130 (40 mg/kg) blocks breast cancer lung metastasis[2].

Chemical Properties

Molecular Weight	420.47
Formula	C25H20N6O
Cas No.	868612-83-3

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 90.0 mg/mL (214.0 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3783 mL	11.8915 mL	23.7829 mL	118.9145 mL
5 mM	0.4757 mL	2.3783 mL	4.7566 mL	23.7829 mL
10 mM	0.2378 mL	1.1891 mL	2.3783 mL	11.8915 mL
20 mM	0.1189 mL	0.5946 mL	1.1891 mL	5.9457 mL
50 mM	0.0476 mL	0.2378 mL	0.4757 mL	2.3783 mL
100 mM	0.0238 mL	0.1189 mL	0.2378 mL	1.1891 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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