Polθ-IN-9

Overview

Polθ-IN-9 is an orally active Polθ polymerase inhibitor ( IC 50 = 9.6 nM, K d = 47.5 nM). Polθ-IN-9 shows remarkable selectivity with no inhibitory activity against other human DNA polymerases, including Pol α, Pol ε, Pol γ, Pol λ, and Pol μ. Polθ-IN-9 exhibits strong antiproliferative activity in DLD1 BRCA2 KO cells (IC 50 = 2.9 μM), and high sensitivity to MDA-MB-436 cells (IC 50 = 4.9 μM). Polθ-IN-9 increases DNA damage accumulation, induces γH2AX levels, and inhibits tumor growth in combination with Olaparib ( HY-10162 ), in the MDA-MB-436 xenograft model. Polθ-IN-9 can be used for the research of homologous recombination (HR)-deficient cancers such as breast cancer .

Application

Products | Products > Disease Areas > Cancer | Products > Disease Areas > Breast Cancer | Products > Signaling Pathways > Cell Cycle/DNA Damage | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Signaling Pathways > DNA/RNA Synthesis

Product Information

• Catalog No.: HY-179413
• CAS No.: 3050552-13-8
• Molecular Formula: C30H31ClF5N5O2
• Molecular Weight: 624.04
• Purity: 99.98%
• Storage: Please store the product under the recommended conditions in the Certificate of Analysis.

Source

Original product source