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AZ 12799734

Catalog No. T35896Cas No. 1117684-36-2
Alias 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.

AZ 12799734

AZ 12799734

Purity: 98.23%
Catalog No. T35896Alias AZ12799734Cas No. 1117684-36-2
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.
Pack SizePriceAvailabilityQuantity
5 mg$113In Stock
10 mg$185In Stock
25 mg$397In Stock
50 mg$662In Stock
100 mg$926In Stock
500 mg$1,850In Stock
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Purity:98.23%
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Product Introduction

Bioactivity
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
TGFβRI:47 nM, BMPR1A:40 μM (Kd), ALK1:7.1 μM (Kd), ALK5:0.74 μM (Kd), ALK6:0.017 μM (Kd), ACVR1:6.2 μM (Kd), ALK4:1 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].
AliasAZ12799734
Chemical Properties
Molecular Weight370.43
FormulaC18H18N4O3S
Cas No.1117684-36-2
Storage & Solubility Information
Storagekeep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 80 mg/mL (215.97 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6996 mL13.4978 mL26.9957 mL134.9783 mL
5 mM0.5399 mL2.6996 mL5.3991 mL26.9957 mL
10 mM0.2700 mL1.3498 mL2.6996 mL13.4978 mL
20 mM0.1350 mL0.6749 mL1.3498 mL6.7489 mL
50 mM0.0540 mL0.2700 mL0.5399 mL2.6996 mL
100 mM0.0270 mL0.1350 mL0.2700 mL1.3498 mL

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