An orally bioavailable inhibitor of PARP1 and PARP2 (IC50s = 3.8 and 2.1 nM

MK-4827 (tosylate) – 5 mg

Brand:
Cayman
CAS:
1038915-73-9
Storage:
-20
UN-No:
De Minimis - 3077 / 9

MK-4827 is an orally bioavailable inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 3.8 and 2.1 nM, respectively).{34138} It inhibits the proliferation of cancer cells carrying the breast cancer mutations BRCA1 and BRCA2 in vitro (IC50 values range from 10-100 nM) and has efficacy alone against a xenograft of BRCA1-deficient cancer in mice.{34138,20554} MK-4827 sensitizes human lung and breast cancer xenografts to radiation in mice.{34140} Formulations containing MK-4827 are effective against ovarian cancer, particularly in platinum-sensitive, recurrent ovarian cancer.{34139}  

 

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Description

An orally bioavailable inhibitor of PARP1 and PARP2 (IC50s = 3.8 and 2.1 nM, respectively); inhibits the proliferation of BRCA1 and BRCA2 mutant cancer cells in vitro (IC50s = 10-100 nM) and has efficacy alone against a xenograft of BRCA1-deficient cancer in mice

Formal name: 2-[4-(3S)-3-piperidinylphenyl]-2H-indazole-7-carboxamide, 4-methylbenzenesulfonate

Synonyms:  Niraparib tosylate

Molecular weight: 492.6

CAS: 1038915-73-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|DNA Repair Enzymes||Research Area|Cancer|DNA Damage and Repair|PARP

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