RTx-152

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].

Product Specifications

CAS Number

[3035072-48-8]

UNSPSC

12352005

Target

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

Purity

99.71

Solubility

DMSO : 50 mg/mL (ultrasonic)

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 Formula

C20H16F7N3O3

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.