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Polθ-IN-9

CAT: 0804-HY-179413Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-179413Size:1 Each
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Description
Polθ-IN-9 is an orally active Polθ polymerase inhibitor (IC50 = 9.6 nM, Kd = 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 (IC50 = 2.9 μM), and high sensitivity to MDA-MB-436 cells (IC50 = 4.9 μM). Polθ-IN-9 increases DNA damage accumulation, induces γH2AX levels, and inhibits tumor growth in combination with Olaparib , 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[1].
CAS Number
3050552-13-8
UNSPSC
12352005
Target
DNA/RNA Synthesis
Related Pathways
Cell Cycle/DNA Damage
Field of Research
Cancer
Smiles
COCCN1CCN(CC1)C2=CC=C3N([C@@H](CC3=C2)C(N(C)C4=CC(Cl)=C(C=C4F)F)=O)C5=CC(C(F)(F)F)=CC(C)=N5
Molecular Formula
C30H31ClF5N5O2
Molecular Weight
624.04
References & Citations
[1]Yu Z, et al. Rational Design and Biological Evaluation of a Novel Polθ Polymerase Inhibitor for Synergistic Targeting of HR-Deficient Cancers. J Med Chem. 2025 Nov 27;68 (22) :23801-23824.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
DNA Polymerases

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