AZ 12799734

SKU: orb1694221

Description

AZ 12799734 is a potent, selective, and orally bioavailable dual inhibitor of TGFBR1/ALK5, also modulating BMP and TGFβ signaling pathways. This small molecule is utilized in cancer research to investigate tumor progression and metastasis in both cellular assays and animal models.

Research Area

Cardiovascular Research, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1117684-36-2
• MW: 370.43
• Purity: 98.95% (May vary between batches)
• Formula: C₁₈H₁₈N₄O₃S
• SMILES: O(C=1C=C(NC2=CC=C(S(N)(=O)=O)C=C2)N=CC1)C3=C(C)N=C(C)C=C3
• Target: ALK,TGF-beta/Smad
• Solubility: DMSO:80 mg/mL (215.97 mM)

Bioactivity

• Target IC50:
  ALK4:1 μM (Kd)|TGFβRI:47 nM|ALK5:0.74 μM (Kd)|ALK1:7.1 μM (Kd)|ALK6:0.017 μM (Kd)|ACVR1:6.2 μM (Kd)|BMPR1A:40 μM (Kd)
• 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. 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.
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• In Vitro:
  Inhibiting ligand-activated SMAD3/4 transcription, AZ12799734. AZ12799734 (10 nM; 24 h) inhibits phosphorylation of both SMAD1 and SMAD2. AZ12799734 (500 nM; 36 h) inhibits TGFβ-induced migration in HaCaT epithelial cells.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ALK5, AZ12799734, AZ-12799734, AZ 12799734

Compound Identifiers

PubChem CID

25192277