| Bioactivity | 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]. |
| Invitro | AZ12799734 inhibits ligand activated SMAD3/4 transcription[1].AZ12799734 (10 nM; 24 h) inhibits phosphorylation of both SMAD1 and SMAD2[1].AZ12799734 (500 nM; 36 h) inhibits TGFβ-induced migration in HaCaT epithelial cells[1]. Western Blot Analysis[1] Cell Line: |
| 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: |
| Name | AZ12799734 |
| CAS | 1117684-36-2 |
| Formula | C18H18N4O3S |
| Molar Mass | 370.43 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. [2]. Anderton MJ, et al. Induction of heart valve lesions by small-molecule ALK5 inhibitors. Toxicol Pathol. 2011 Oct;39(6):916-24. |
AZ12799734
CAS: 1117684-36-2 F: C18H18N4O3S W: 370.43
AZ12799734 is a selective, orally active TGFBR1 kinase inhibitor with an IC50 of 47 nM. AZ12799734 is also a pan BMP and
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