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AZ12601011

Catalog No. T10426Cas No. 2748337-86-0

AZ12601011 is a highly potent and selective inhibitor of the TGFBR1 kinase, administered orally. It displays an IC50 of 18 nM and a Kd of 2.9 nM. By selectively targeting ALK4, TGFBR1, and ALK7, AZ12601011 effectively inhibits the phosphorylation of SMAD2. Additionally, it has been shown to hinder the growth and metastasis of mammary tumors [1].

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Pack Size	Price	Availability
25 mg	$985	10-14 weeks
50 mg	$1,280	10-14 weeks
100 mg	$1,780	10-14 weeks

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Product Introduction

Bioactivity

Description	AZ12601011 is a highly potent and selective inhibitor of the TGFBR1 kinase, administered orally. It displays an IC50 of 18 nM and a Kd of 2.9 nM. By selectively targeting ALK4, TGFBR1, and ALK7, AZ12601011 effectively inhibits the phosphorylation of SMAD2. Additionally, it has been shown to hinder the growth and metastasis of mammary tumors [1].
In vitro	AZ12601011 (0.01-10 μM; for 20 minutes) entirely inhibits Phosphorylation of SMAD2 [1]. AZ12601011 (0.01 μM-10 μM) inhibits the activity of ALK4, ALK7 and TGFBR1 [1]. AZ12601011 inhibits 4T1 cells growth in vitro (IC 50 =0.4μM) [1]. Western Blot Analysis [1] Cell Line: NIH3T3, HaCaT, C2C12, T47D cells Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM Incubation Time: 20 minutes Result: Completely inhibited Phosphorylation of SMAD2.
In vivo	AZ12601011 (50mg/kg; oral gavage; twice daily; for 25 days) significantly suppresses tumor growth and metastasis in vivo [1]. Administered to female BALB/c mice weighing over 18g and bearing tumors [1] at a dosage of 50mg/kg through oral gavage twice daily for a duration of 25 days, the compound effectively hindered both tumor development and migration.

Chemical Properties

Molecular Weight	313.36
Formula	C19H15N5
Cas No.	2748337-86-0

Storage & Solubility Information

Storage

keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5 mg/mL (15.96 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.1912 mL	15.9561 mL	31.9122 mL	159.5609 mL
5 mM	0.6382 mL	3.1912 mL	6.3824 mL	31.9122 mL
10 mM	0.3191 mL	1.5956 mL	3.1912 mL	15.9561 mL

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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

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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