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Chemical Structure
Chemical Structure
Chemical Structure

A-674563 (free base) [552325-73-2]

Research Use Only
AG-CR1-3680
AdipoGen Life Sciences
CAS Number552325-73-2
Product group Chemicals
Estimated Purity>98%
Molecular Weight358.4
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Packing Size
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Overview

  • Supplier
    AdipoGen Life Sciences
  • Product Name
    A-674563 (free base) [552325-73-2]
  • Delivery Days Customer
    10
  • CAS Number
    552325-73-2
  • Certification
    Research Use Only
  • Estimated Purity
    >98%
  • Hazard Information
    Warning
  • Molecular Formula
    C22H22N4O
  • Molecular Weight
    358.4
  • Scientific Description
    A-674563 is a potent, ATP-competitive, reversible and orally available Akt1 inhibitor with an IC50 of 11nM. Binds to the ATP site of the AKT kinase domain, inhibiting AKT-catalyzed phosphorylation activity. Also inhibits PKA and CDK2 with IC50 values of 16nM and 46nM, respectively. 10- to >1,800-fold selective for Akt1 versus additional kinases in the CMGC, CAMK and TK families. Anticancer compound. Reduces phosphorylation of Akt downstream targets in cells and slows proliferation of tumor cells in vitro with an EC50 value of 0.4microM. Shown to decrease tumor growth in mouse tumor xenograft models. Decreased sphingosine kinase 1 (SphK1) activity in AML cells to deplete pro-survival sphingosine-1-phosphate (S1P) and boost pro-apoptotic ceramide production. - Chemical. CAS: 552325-73-2. Formula: C22H22N4O. MW: 358.4. Synthetic. A-674563 is a potent, ATP-competitive, reversible and orally available Akt1 inhibitor with an IC50 of 11nM. Binds to the ATP site of the AKT kinase domain, inhibiting AKT-catalyzed phosphorylation activity. Also inhibits PKA and CDK2 with IC50 values of 16nM and 46nM, respectively. 10- to >1,800-fold selective for Akt1 versus additional kinases in the CMGC, CAMK and TK families. Anticancer compound. Reduces phosphorylation of Akt downstream targets in cells and slows proliferation of tumor cells in vitro with an EC50 value of 0.4microM. Shown to decrease tumor growth in mouse tumor xenograft models. Decreased sphingosine kinase 1 (SphK1) activity in AML cells to deplete pro-survival sphingosine-1-phosphate (S1P) and boost pro-apoptotic ceramide production.
  • SMILES
    CC1=NNC2=CC=C(C3=CC(OC[C@H](CC4=CC=CC=C4)N)=CN=C3)C=C21
  • Storage Instruction
    2°C to 8°C
  • UNSPSC
    12352200

References

  • Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo: Y. Luo, et al.; Mol. Cancer Ther. 4, 977 (2005)