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SML4217

M324

≥98% (HPLC), powder, rucaparib metabolite

Synonym(s):

4-(8-Fluoro-3,4,5,6-tetrahydro-6-oxo-1H-pyrrolo[4,3,2-ef][2]benzazepin-2-yl)benzoic acid, Rucaparib metabolite M324, rucaparib carboxy metabolite

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About This Item

Empirical Formula (Hill Notation):
C18H13FN2O3
CAS Number:
1577998-89-0
Molecular Weight:
324.31
UNSPSC Code:
12352203
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

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.

Pictograms

Exclamation mark
GHS07

Signal Word

Warning

Hazard Codes

H302,H315,H319

Hazard Classifications

Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2

Storage Class

11 - Combustible Solids

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

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