GTx-134

• Description:

  GTx-134 is a dual insulin-like growth factor 1 receptor/insulin receptor (IGF-1R/IR) inhibitor with an IC50 values for IGF-1R and IR of 97 and 187 nM respectively. GTx-134 inhibits the autophosphorylation of IGF-1R and its downstream signaling pathway (Akt), thereby blocking the proliferation and survival signals of tumor cells. GTx-134 has broad-spectrum inhibitory activity against multiple myeloma cell lines and can induce apoptosis in sensitive cells. GTx-134 significantly inhibits tumor growth in mice with MM1.S cell transplantation. GTx-134 works in synergy with existing therapies (such as protease preparations, immunomodulators) . GTx-134 can be used in high-risk myeloma research[1].

• UNSPSC:

  12352005

• Target:

  Akt; Apoptosis; IGF-1R; Insulin Receptor

• Related Pathways:

  Apoptosis; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Smiles:

  CC(C=C(C=C1)C)=C1OC[C@H](O)CNC2=C(C(NC=C2)=O)C3=NC(C=C4C(C(N(C5CCN(CC5)CCS(C)(=O)=O)C4)=O)=C6)=C6N3

• Molecular Formula:

  C33H40N6O6S

• Molecular Weight:

  648.77

• References & Citations:

  [1]Liang SB, et al. Molecular target characterization and antimyeloma activity of the novel, insulin-like growth factor 1 receptor inhibitor, GTx-134. Clin Cancer Res. 2011 Jul 15;17 (14) :4693-704.

• Shipping Conditions:

  Room temperature

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• CAS Number:

  [1008448-19-8]