ChemicalBook CAS DataBase List 1117684-36-2

1117684-36-2

Name	4-({4-[(2,6-dimethylpyridin-3-yl)oxy]pyridin-2-yl}amino)benzenesulfonamide
CAS	1117684-36-2
Molecular Formula	C18H18N4O3S
MDL Number	MFCD26397939
Molecular Weight	370.43
MOL File	1117684-36-2.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	Soluble in DMSO
form	Solid
color	White to off-white

Safety Data

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Hazard Information

Uses

AZ12799734 is a selective, orally active TGFBR1 kinase inhibitor with an IC50 of 47 nM. AZ12799734 is also a pan BMP and TGFβ inhibitor[1].

Biochem/physiol Actions

AZ12799734 is an orally active TGF-β type I receptors active site inhibitor (ALK1/2/3/4/5/6 Kd = 7.1/6.2/40/1/0.74/0.017 μM) that inhibits ALK5-dependent Smad2 nuclear translocation upon TGF-β1 stimulation (IC50 = 17 nM; MDA-MB-468), as well as ALK1/2/3/6-mediated Smad1 and ALK4/5/7-mediated Smad2 phosphorylation (10 μM; NIH3T3 expressing respective constitutively active receptors). AZ12799734 oral administration in rats results in heart valve lesions (200 mg/kg/day for 5 days) and physeal dysplasia (400 mg/kg/day for 6 days), consistent with a critical role of ALK5 in maintaining the integrity of heart valve and physis.

in vivo

AZ12799734 (0-400 mg/kg/day; p.o.; 3-7 days) induces histopathologic heart valve lesions in rat^[2].
AZ12799734 (50 mg/kg; p.o.; once) shows total and free pharmacokinetic (PK) levels in the nude mouse with time over in vitro IC₅₀ of 0.01885 μM^[1].

Animal Model:	Ten-week-old female HsdHan:WIST rats^[2]
Dosage:	200 and 400 mg/kg/day
Administration:	Oral, 3-7 days
Result:	Hemorrhage into the heart valves was evident at low magnification and the normal architecture of the leaflet was replaced by hemorrhage. Increased valvular interstitial cells in size and number and shows increased cytoplasm, an enlarged round to spindeloid nucleus, and frequently undergoing mitosis.

Animal Model:	Female BALB/c mice^[1]
Dosage:	50 mg/kg
Administration:	Oral administration (Pharmacokinetic Analysis)
Result:	Showed total and free pharmacokinetic (PK) levels with time over in vitro IC₅₀ of 0.01885 μM.

IC 50

TGFBR1: 47 nM (IC₅₀); ALK6: 0.017 μM (Kd); ALK5: 0.74 μM (Kd); ALK4: 1 μM (Kd); ACVR1: 6.2 μM (Kd); ALK1: 7.1 μM (Kd); BMPR1A: 40 μM (Kd); BMP

storage

Store at -20°C

References

[1] 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. DOI:10.1124/mol.118.112946
[2] Anderton MJ, et al. Induction of heart valve lesions by small-molecule ALK5 inhibitors. Toxicol Pathol. 2011 Oct;39(6):916-24. DOI:10.1177/0192623311416259

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