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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 Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $113 | In Stock | |
10 mg | $185 | In Stock | |
25 mg | $397 | In Stock | |
50 mg | $662 | In Stock | |
100 mg | $926 | In Stock | |
500 mg | $1,850 | In Stock |
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]. |
Alias | 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 | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (215.97 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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