3068829-46-6
Chemical Structure
Polθ-IN-10
- CAS No.: 3068829-46-6
- Formula:C27H24F4N6O3
- Molecular Weight:556.51
InChIKey: CILXGQYVAOPHCR-NRFANRHFSA-N
SMILES: O=C(N(CC#CC1=NN=C(C=C1)C(O)(C)C)C2=CC=C(C=C2)F)[C@@H](N3C4=NC(C)=CC(C(F)(F)F)=C4)CNC3=O
Biological Activity: Polθ-IN-10 is an orally active Polθ-pol inhibitor (with a human IC50 of 1.3 nM) that exhibits oral bioavailability in mice and rats. Polθ-IN-10 binds to the allosteric site of Polθ-pol, disrupts the microhomology-mediated end-joining DNA repair pathway, and inhibits CYP2C9 (IC50=1.63 μM). Polθ-IN-10 selectively inhibits the proliferation of HR-deficient cancer cells and induces apoptosis. Polθ-IN-10 is applicable to the research of HR-deficient cancers[1].
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Polθ-IN-10 | Polθ-IN-10 is an orally active Polθ-pol inhibitor (with a human IC50 of 1.3 nM) that exhibits oral bioavailability in mice and rats. Polθ-IN-10 binds to the allosteric site of Polθ-pol, disrupts the microhomology-mediated end-joining DNA repair pathway, and inhibits CYP2C9 (IC50=1.63 μM). Polθ-IN-10 selectively inhibits the proliferation of HR-deficient cancer cells and induces apoptosis. Polθ-IN-10 is applicable to the research of HR-deficient cancers. | |||||||||||||||||||||
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