3045467-32-8
Chemical Structure
POLQ-IN-2
- CAS No.: 3045467-32-8
- Formula:C29H33ClN6O2
- Molecular Weight:533.06
InChIKey: ANRIVRGAQRHMTI-UHFFFAOYSA-N
SMILES: CC1(OC2=C3N=C(C4=CC=C(OCCN5CCN(C)CC5)C=C4Cl)N(CC6=CC=CC=C6)C3=NC=N2)CC1
Biological Activity: POLQ-IN-2 is an orally active allosteric inhibitor of the DNA polymerase theta (POLQ) domain. POLQ-IN-2 has an IC50 < 0.003 μM against the human target. POLQ-IN-2 inhibits DNA polymerase activity and microhomology-mediated end joining (MMEJ), and shows selective antiproliferative activity in homologous recombination repair-deficient cells, with low activity in repair-proficient cells. POLQ-IN-2 enhances the antiproliferative activity of Olaparib (HY-10162) in homologous recombination repair-deficient cells, and its combination with Olaparib produces tumor regression in a BRCA2-deficient xenograft model. POLQ-IN-2 can be used for research on BRCA2-deficient colorectal cancer[1].
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POLQ-IN-2 | POLQ-IN-2 is an orally active allosteric inhibitor of the DNA polymerase theta (POLQ) domain. POLQ-IN-2 has an IC50 < 0.003 μM against the human target. POLQ-IN-2 inhibits DNA polymerase activity and microhomology-mediated end joining (MMEJ), and shows selective antiproliferative activity in homologous recombination repair-deficient cells, with low activity in repair-proficient cells. POLQ-IN-2 enhances the antiproliferative activity of Olaparib (HY-10162) in homologous recombination repair-deficient cells, and its combination with Olaparib produces tumor regression in a BRCA2-deficient xenograft model. POLQ-IN-2 can be used for research on BRCA2-deficient colorectal cancer. | |||||||||||||||||||||
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