Polθ-IN-9

SKU: orb3174197

Description

Polθ-IN-9 is an orally active inhibitor of Polθ polymerase with an IC50 of 9.6 nM and a Kd of 47.5 nM. It demonstrates remarkable selectivity, showing no inhibitory activity against other human DNA polymerases, such as Pol α, Pol ε, Pol γ, Pol λ, and Pol μ. In DLD1 BRCA2 KO cells, Polθ-IN-9 exhibits potent antiproliferative activity with an IC50 of 2.9 μM, and it is highly sensitive to MDA-MB-436 cells with an IC50 of 4.9 μM. In MDA-MB-436 xenograft tumor models, the combination of Polθ-IN-9 with Olaparib enhances DNA damage accumulation, increases γH2AX levels, and inhibits tumor growth. Polθ-IN-9 is useful in studying homologous recombination (HR)-deficient cancers such as breast cancer.

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 3050552-13-8
• MW: 624.05
• Formula: C₃₀H₃₁ClF₅N₅O₂
• SMILES: C(N(C)C1=C(F)C=C(F)C(Cl)=C1)(=O)[C@H]2N(C=3C(C2)=CC(=CC3)N4CCN(CCOC)CC4)C5=CC(C(F)(F)F)=CC(C)=N5
• Target: DNA/RNA Synthesis

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

DNA/RNA Synthesis