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AZ12601011

Catalog No. T10426 CAS 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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AZ12601011, CAS 2748337-86-0

Pack Size	Availability	Price/USD
25 mg	10-14 weeks	$ 985.00
50 mg	10-14 weeks	$ 1,280.00
100 mg	10-14 weeks	$ 1,780.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

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Storage & Solubility Information

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].
Targets&IC50	ALK4:, TGFβRI:18 nM, TGFβRI:2.9 nM (kd)
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.

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

Storage

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

Solubility Information

DMSO: 5 mg/mL (15.96 mM), Sonication is recommended.

References and Literature

1. Spender LC, et al. Preclinical Evaluation of AZ12601011 and AZ12799734, Inhibitors of Transforming Growth Factor βSuperfamily Type 1 Receptors. Mol Pharmacol. 2019 Feb;95(2):222-234.

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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

AZ12601011 2748337-86-0 Angiogenesis Tyrosine Kinase/Adaptors ALK AZ-12601011 AZ 12601011 inhibitor inhibit

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