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AZ 12799734

Catalog No. T35896 CAS 1117684-36-2

Synonyms: AZ12799734

AZ 12799734 is an orally active, selective and potent dual inhibitor of TGFBR1 and ALK5 with inhibitory effects on BMP and TGFβ for the study of tumours.

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AZ 12799734, CAS 1117684-36-2

Pack Size	Availability	Price/USD
5 mg	In stock	$ 113.00
10 mg	In stock	$ 185.00
25 mg	In stock	$ 397.00
50 mg	In stock	$ 662.00
100 mg	In stock	$ 926.00
500 mg	In stock	$ 1,850.00

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Purity: 98.23%

Biological Description

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Description	AZ 12799734 is an orally active, selective and potent dual inhibitor of TGFBR1 and ALK5 with inhibitory effects on BMP and TGFβ for the study of tumours.
Targets&IC50	ACVR1:6.2 μM (Kd), ALK5:0.74 μM (Kd), BMPR1A:40 μM (Kd), ALK1:7.1 μM (Kd), ALK4:1 μM (Kd), TGFβRI:47 nM, ALK6:0.017 μM (Kd)
In vitro	Inhibiting ligand-activated SMAD3/4 transcription, AZ12799734[2]. AZ12799734 (10 nM; 24 h) inhibits phosphorylation of both SMAD1 and SMAD2[2]. AZ12799734 (500 nM; 36 h) inhibits TGFβ-induced migration in HaCaT epithelial cells[2].
In vivo	Inducing histopathologic heart valve lesions in rats, AZ12799734 is administered orally at doses ranging from 0 to 400 mg/kg/day for 3-7 days[1]. At a single oral dose of 50 mg/kg, AZ12799734 shows total and free pharmacokinetic (PK) levels in nude mice over time, exceeding the in vitro IC50 of 0.01885 μM[2].

Synonyms	AZ12799734
Molecular Weight	370.43
Formula	C18H18N4O3S
CAS No.	1117684-36-2

Storage

keep away from direct sunlight

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

Solubility Information

DMSO: 80 mg/mL (215.97 mM), Sonication is recommended.

References and Literature

1. Anderton MJ, et al. Induction of heart valve lesions by small-molecule ALK5 inhibitors. Toxicol Pathol. 2011 Oct;39(6):916-24. 2. Spender LC, et al. Preclinical Evaluation of AZ12601011 and AZ12799734, Inhibitors of Transforming Growth Factor β Superfamily Type 1 Receptors. Mol Pharmacol. 2019 Feb;95(2):222-234. 3. Spender et al (2019) Preclinical evaluation of AZ12601011 and AZ12799734, inhibitors of transforming growth factor β superfamily type 1 receptors. Mol.Pharmacol. 95 222 PMID:30459156

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Inhibitor Library

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Related compounds with same targets

LDN-212854 Alectinib SB 525334 Repotrectinib AZ12601011 Lorlatinib GW788388 Crizotinib hydrochloride

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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

AZ 12799734 1117684-36-2 Angiogenesis Tyrosine Kinase/Adaptors ALK AZ12799734 AZ-12799734 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.