GTx-134
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].
Product Specifications
CAS Number
[1008448-19-8]
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
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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