Application
M324 may be used to study the inhibition properties of M324, potentially linking it to enhanced efficacy in cancer treatment.
Biochem/physiol Actions
M324 is a major (oxidative) metabolite of PARP1 inhibitor rucaparib which reaches plasma concentration levels comparable to those of the parent drug. But it retains weaker PARP inhibition activities (IC50 = 550 nM) than parent rucaparib (Ki = 1.4 and 0.17 nM PARP-1 and PARP-2 respectively). M324 has a differential kinase polypharmacology profile than parent drug. M324 inhibits PLK2 (IC50 = 591 nM) and GSK3A (IC50 = 579 nM) at clinical concentrations. Rucaparib and M324 exhibit synergistic effects in viability of prostate cancer cell lines. Also, M324 reduces α-synuclein accumulation in iPSC dopamine neurons in Parkinson’s disease models.
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | 2-8°C |
