AZ12601011 B

CAS No. 2748337-86-0

AZ12601011 B( —— )

Catalog No. M32795 CAS No. 2748337-86-0

AZ12601011 is an orally active, selective and potent TGFBR1 kinase inhibitor.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
1 mL x 10 mM in DMSO 258 In Stock
5MG 235 In Stock
10MG 376 In Stock
25MG 729 In Stock
50MG 1070 In Stock
100MG 1479 In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    AZ12601011 B
  • Note
    Research use only, not for human use.
  • Brief Description
    AZ12601011 is an orally active, selective and potent TGFBR1 kinase inhibitor.
  • Description
    AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .
  • In Vitro
    AZ12601011 (0.01-10 μM; for 20 minutes) completely inhibits Phosphorylation of SMAD2 . AZ12601011 (0.01 μM-10 μM) inhibits the activity of ALK4, ALK7 and TGFBR1. AZ12601011 inhibits 4T1 cells growth in vitro (IC50=0.4μM) . Western Blot Analysis Cell Line:NIH3T3, HaCaT, C2C12, T47D cells Concentration:0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM Incubation Time:20 minutes Result:Completely inhibited Phosphorylation of SMAD2.
  • In Vivo
    AZ12601011 (50mg/kg; oral gavage; twice daily; for 25 days) inhibits tumour growth and metastasis in vivo. Animal Model:Female BALB/c mice at greater than 18g with tumour Dosage:50mg/kg Administration:Oral gavage; twice daily; for 25 days Result:Inhibited tumour growth and metastasis in vivo.
  • Synonyms
    ——
  • Pathway
    Angiogenesis
  • Target
    ALK
  • Recptor
    ALK | TGF-beta/Smad
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2748337-86-0
  • Formula Weight
    313.36
  • Molecular Formula
    C19H15N5
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 5 mg/mL (15.96 mM; Ultrasonic )
  • SMILES
    N=1C=CC2=C(C1)C=CN2C3=NC(=NC4=C3CCC4)C5=NC=CC=C5
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Spender LC, et al. Preclinical Evaluation of AZ12601011 and AZ12799734, Inhibitors of Transforming Growth Factor βSuperfamily Type 1 Receptors. Mol Pharmacol. 2019 Feb;95(2):222-234.?
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