AZ12601011

CAS No. ——

AZ12601011( AZ-12601011 | AZ 12601011 )

Catalog No. M16993 CAS No. ——

AZ12601011 (AZ-12601011) is a potent, selective inhibitor of ALK4, ALK7 and TGFBR1 (Kd=2.9 nM).

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    AZ12601011
  • Note
    Research use only, not for human use.
  • Brief Description
    AZ12601011 (AZ-12601011) is a potent, selective inhibitor of ALK4, ALK7 and TGFBR1 (Kd=2.9 nM).
  • Description
    AZ12601011 (AZ-12601011) is a potent, selective inhibitor of ALK4, ALK7 and TGFBR1 (Kd=2.9 nM), inhibits TGFβ-induced reporter activity with IC50 of 18 nM; inhibits TGFBR1 kinase activity (competition binding) with Kd of 2.9 nM, shows some inhibitory activity against the related receptors ALK4 and BMPR1B, but shows only weakly activity against ALK1, ALK2 and BMPR1A in in vitro kinase assays; AZ12601011 is a more effective inhibitor of TGFβ-induced reporter activity than SB-431542 (IC50=84nM) and LY2157299 (galunisertib) (IC50=380nM), inhibits phosphorylation of SMAD2 via the type 1 receptors ALK4, TGFBR1 and ALK7; AZ12601011 is highly effective at inhibiting basal and TGFβ-induced migration of HaCaT keratinocytes, inhibits tumour growth and metastasis to the lungs in a 4T1 syngeneic orthotopic mammary tumour model.
  • In Vitro
    ——
  • In Vivo
    ——
  • Synonyms
    AZ-12601011 | AZ 12601011
  • Pathway
    TGF-beta/Smad
  • Target
    TGFBR
  • Recptor
    TGFBR
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    ——
  • Formula Weight
    313.364
  • Molecular Formula
    C19H15N5
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    ——
  • Chemical Name
    2-(pyridin-2-yl)-4-(1H-pyrrolo[3,2-c]pyridin-1-yl)-6,7-dihydro-5H-cyclopenta[d]pyrimidine

Shipping & Storage Information

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

Reference

1. Spender LC, et al. Mol Pharmacol. 2018 Nov 20. pii: mol.118.112946. doi: 10.1124/mol.118.112946.
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