| Identification | Back Directory | [Name]
AZD2461 | [CAS]
1174043-16-3 | [Synonyms]
CS-739
AZD2461
AZD 2461, >=98%
AZD2461 USP/EP/BP
4-[4-Fluoro-3-[(4-methoxypiperidin-1-yl)carbonyl]benzyl]phthalazin-1(2H)-one
4-[[4-fluoro-3-(4-methoxypiperidine-1-carbonyl)phenyl]methyl]-2H-phthalazin-1-one
4-[[4-Fluoro-3-[(4-methoxy-1-piperidinyl)carbonyl]phenyl]methyl]-1(2H)-phthalazinone
1(2H)-Phthalazinone, 4-[[4-fluoro-3-[(4-methoxy-1-piperidinyl)carbonyl]phenyl]methyl]- | [Molecular Formula]
C22H22FN3O3 | [MDL Number]
MFCD24386811 | [MOL File]
1174043-16-3.mol | [Molecular Weight]
395.43 |
| Chemical Properties | Back Directory | [density ]
1.33±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
insoluble in H2O; ≥16.35 mg/mL in DMSO; ≥45.2 mg/mL in EtOH with ultrasonic | [form ]
powder | [pka]
12.07±0.40(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
4-[4-Fluoro-3-[(4-methoxypiperidin-1-yl)carbonyl]benzyl]phthalazin-1(2H)-one is a phthalazinone derivative and potential PARP inhibitor. | [Biochem/physiol Actions]
AZD2461, an olaparib analog, is an orally available, potent and selective PARP1 and PARP2 inhibitor that is a poor substrate for drug transporters. AZD2461 exhibits a high efficacy in olaparib-resistant tumors that overexpress P-glycoprotein. | [in vivo]
AZD-2461 (10 mg/kg, p.o.) enhances the antitumor activity of temozolomide in a mouse colorectal xenograft and exhibits low effect on mouse bone marrow cells. However, the increased bone marrow tolerability of AZD-2461 is not seen in rat models[1]. AZD-2461 (0.5% v/w HPMC, p.o.) increases the survival of mice bearing KB1P tumors after short-term treatment, and long-term treatment is well tolerated, but can not lead to tumor eradication[3]. | [IC 50]
PARP2: 2 nM (IC50); PARP1: 5 nM (IC50); PARP3: 200 nM (IC50) | [storage]
Store at -20°C |
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