RTx-152

• UNSPSC Description:

  RTx-152 traps Polθ on DNA and is an allosteric Polθ-pol inhibitor (IC50: 6.2 nM). RTx-152 selectively kills HR-deficient cancer cells, and suppresses PARP inhibitor resistance in multiple genetic backgrounds, including homologous recombination (HR)-proficient cells. RTx-152 selectively kills BRCA2-null cells[1].

• Target Antigen:

  DNA/RNA Synthesis

• Type:

  Reference compound

• Related Pathways:

  Cell Cycle/DNA Damage

• Applications:

  Cancer-programmed cell death

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/rtx-152.html

• Solubility:

  10 mM in DMSO

• Smiles:

  FC(F)(F)C1=CC(N2CCN(C)C2=O)=C(OC(N(C3=CC=C(F)C=C3)C)=O)C(C(F)(F)F)=C1

• Molecular Weight:

  479.35

• References & Citations:

  [1]Fried W, et al. Discovery of a small-molecule inhibitor that traps Polθ on DNA and synergizes with PARP inhibitors. Nat Commun. 2024 Apr 5;15(1):2862.

• Shipping Conditions:

  Room temperature

• Clinical Information:

  No Development Reported

• CAS Number:

  3035072-48-8