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  1. General Info
  2. Effects Info
  3. Reference
Drug Details
01. General Information
Name Niraparib
PubChem CID 24958200
Molecular Weight 320.4g/mol
Synonyms

Niraparib, 1038915-60-4, MK-4827, (S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide, MK4827, UNII-HMC2H89N35, MK 4827 (Base), Niraparib [USAN], HMC2H89N35, 2-{4-[(3s)-piperidin-3-yl]phenyl}-2h-indazole-7-carboxamide, MK 4827, MK-4827 (Niraparib), ZL-2306, JNJ-64091742, 2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide, CHEMBL1094636, CHEBI:176844, DTXSID50146129, Niraparib (USAN), 2-[4-(3S)-3-Piperidinylphenyl]-2H-indazole-7-carboxamide, 2H-INDAZOLE-7-CARBOXAMIDE, 2-(4-(3S)-3-PIPERIDINYLPHENYL)-, (S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide;MK-4827, compound 56 (PMID 19873981), compound 56 [PMID 19873981], Niraparib [USAN:INN], niraparibum, 2-(4-((3S)-piperidin-3-yl)phenyl)indazole-7-carboxamide, 2-(4-(3S)-3-piperidinylphenyl)-2H-indazole-7-carboxamide, 2-(4-((3S)-PIPERIDIN-3-YL)PHENYL)-2H-INDAZOLE-7-CARBOXAMIDE, C19H20N4O, 2H-Indazole-7-carboxamide, 2-[4-(3S)-3-piperidinylphenyl]-; 2-[4-(3S)-3-Piperidinylphenyl]-2H-indazole-7-carboxamide; Niraparib; Zejula; MK-4827, 3JD, Zejula (TN), NIRAPARIB [INN], NIRAPARIB [MI], MK-4827(Niraparib), NIRAPARIB [WHO-DD], GTPL8275, SCHEMBL1421875, DTXCID8068620, Niraparib(MK4827) free base?, AMY4192, EX-A290, L01XX54, MK-4827 (PARP-1), BDBM50316226, MFCD17779309, NSC754355, NSC800020, s2741, AKOS016004869, BCP9000940, CCG-267709, CS-0780, DB11793, MK-4827/MK4827, NSC-754355, NSC-800020, NCGC00346435-01, NCGC00346435-04, NCGC00346435-12, NCGC00346435-13, AC-28447, AS-35248, HY-10619, Akeega (niraparib and abiraterone acetate), BCP0726000077, 5129B, 5142B, NS00072574, D10140, EN300-7364833, A857972, Q25326660, 2H-Indazole-7-carboxamide, 2-[4-(3S)-3-piperidinylphenyl]

Drug Type Small molecule
Formula C₁₉H₂₀N₄O
SMILES C1CC(CNC1)C2=CC=C(C=C2)N3C=C4C=CC=C(C4=N3)C(=O)N
InChI 1S/C19H20N4O/c20-19(24)17-5-1-3-15-12-23(22-18(15)17)16-8-6-13(7-9-16)14-4-2-10-21-11-14/h1,3,5-9,12,14,21H,2,4,10-11H2,(H2,20,24)/t14-/m1/s1
InChIKey PCHKPVIQAHNQLW-CQSZACIVSA-N
CAS Number 1038915-60-4
ChEMBL ID CHEMBL1094636
ChEBI ID CHEBI:176844
TTD ID D0DN0W
Drug Bank ID DB11793
KEGG ID D10140
Toxicity Organism Test Type Route(Dose)
rat LD50 intraperitoneal(165 mg/kg)
mouse LD50 intraperitoneal(254 mg/kg)
rat LD50 oral(322 mg/kg)
Structure 2D-img
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2D MOL 3D MOL
02. Combinatorial Therapeutic Effect(s)
Synergistic Effect
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Enhancing Drug Efficacy
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Combination Pair ID: 756
Pair Name Berberine, Niraparib
Partner Name Berberine
Disease Info [ICD-11: 2C73] Ovarian cancer Investigative
Biological Phenomena Induction-->DNA damage
Gene Regulation Up-regulation Phosphorylation H2AX hsa3014
Down-regulation Expression NR1H4 KEGG ID N.A.
Down-regulation Expression RAD51 hsa5888
In Vitro Model A2780 Ovarian endometrioid adenocarcinoma Homo sapiens (Human) CVCL_0134
HO-8910 Human papillomavirus-related cervical adenocarcinoma Homo sapiens (Human) CVCL_6868
In Vivo Model The animals were subcutaneously inoculated with 1 × 106 A2780 cells (suspended in 100 μl PBS) and six days later the tumor-bearing mice were randomly divided into four groups and were then treated daily by oral gavage with vehicle (sodium carboxymethycellulose, SCMC), berberine (200 mg/kg bodyweight), niraparib (40 mg/kg bodyweight) and berberine (200 mg/kg) in combination with niraparib (40 mg/kg), respectively, for 15 days.
Result The results indicate that by inducing oxidative DNA damage and downregulating HRR in cancer cells berberine is able to further sensitize cancer cells to PARP inhibition. These results demonstrate a potential therapeutic value of combined application of berberine and PARP inhibitors in ovarian cancer treatment.
03. Reference
No. Title Href
1 Berberine induces oxidative DNA damage and impairs homologous recombination repair in ovarian cancer cells to confer increased sensitivity to PARP inhibition. Cell Death Dis. 2017;8(10):e3070. Published 2017 Oct 5. doi:10.1038/cddis.2017.471 Click
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