Compound class:
Synthetic organic
Comment: This compound is reported to exhibit dual functions as a poly ADP-ribose polymerase 1 (PARP1) inhibitor and cyclin-dependent kinase 12 (CDK12) inhibitor [1]. These two enzymes are important components of the DNA damage repair (DDR) response. CDK12 may be overexpressed in aggressive HER2-positive breast cancers. PARP inhibition is an established mechanism that is employed to disrupt DDR in cancer cells, particulary those with existing defects in homologous recombination such as BRCA-mutated breast cancers. Compound 9 was developed to investigate the anti-tumour potential of simultaneous disruption of the activities of these two molecular targets. It acts is a direct inhibitor of PARP1 and reduces expression of CDK12.
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Classification | |
Compound class | Synthetic organic |
IUPAC Name |
4-[(4-fluoro-3-{2-[3-(piperidin-1-yl)propoxy]-5H,6H,7H,8H-pyrido[4,3-d]pyrimidine-6-carbonyl}phenyl)methyl]-1,2-dihydrophthalazin-1-one |
Database Links | |
GtoPdb PubChem SID | 483123354 |
PubChem CID | 168433309 |
Search Google for chemical match using the InChIKey | FGGDDPHGBCQQLG-UHFFFAOYSA-N |
Search Google for chemicals with the same backbone | FGGDDPHGBCQQLG |
UniChem Compound Search for chemical match using the InChIKey | FGGDDPHGBCQQLG-UHFFFAOYSA-N |
UniChem Connectivity Search for chemical match using the InChIKey | FGGDDPHGBCQQLG-UHFFFAOYSA-N |