AZ12601011

SKU: orb1710355

Description

AZ12601011 is a potent, selective, and orally bioavailable TGF-β receptor 1 (TGFBR1) kinase inhibitor. It binds directly to TGFBR1, blocking Smad3 signaling, which underlies its demonstrated activity in reducing inflammatory cytokine release and inhibiting tumor growth in breast cancer models, as well as its potential in preventing renal fibrosis.

Research Area

Cardiovascular Research, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2748337-86-0
• MW: 313.36
• Purity: 99.61% (May vary between batches)
• Formula: C₁₉H₁₅N₅
• SMILES: N=1C=CC2=C(C1)C=CN2C3=NC(=NC4=C3CCC4)C5=NC=CC=C5
• Target: ALK,TGF-beta/Smad
• Solubility: DMSO:4 mg/mL (12.76 mM)

Bioactivity

• Target IC50:
  TGFBR1:18 nM|TGFBR1:2.9 nM (Kd)|ALK4:|TGFβRI:18 nM|TGFβRI:2.9 nM (kd)
• In Vivo:
  AZ12601011 (50mg/kg; oral gavage; twice daily; for 25 days) significantly suppresses tumor growth and metastasis in vivo . Administered to female BALB/c mice (weight >18g) bearing tumors, the compound effectively hinders both tumor development and migration.
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• In Vitro:
  AZ12601011 (0.01-10 μM; for 20 minutes) entirely inhibits phosphorylation of SMAD2 and the activity of ALK4, ALK7, and TGFBR1. It also inhibits 4T1 cell growth in vitro (IC50 = 0.4 μM). Western Blot Analysis shows complete inhibition of SMAD2 phosphorylation in NIH3T3, HaCaT, C2C12, and T47D cells at concentrations of 0.01-10 μM after 20 minutes of incubation.
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Storage & Handling

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

Alternative Names

ALK4, AZ 12601011, AZ12601011, AZ-12601011, TGF-b/Smad, TGFb, TGF-beta, TGFbeta, TGFbeta/Smad, TGFBR1, Smad, TGF-β/Smad, TGFβR1, TGFβ

Compound Identifiers

PubChem CID

137796280