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SML1858

Sigma-Aldrich

AZD2461

≥98% (HPLC)

Sinonimo/i:

4-[4-Fluoro-3-[(4-methoxypiperidin-1-yl)carbonyl]benzyl]phthalazin-1(2H)-one, 4-[[4-Fluoro-3-[(4-methoxy-1-piperidinyl)carbonyl]phenyl]methyl]-1(2H)-phthalazinone, AZD 2461, AZD-2461

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About This Item

Formula empirica (notazione di Hill):
C22H22FN3O3
Numero CAS:
1174043-16-3
Peso molecolare:
395.43
Numero MDL:
MFCD24386811
Codice UNSPSC:
12352200
NACRES:
NA.77

Livello qualitativo

100

Saggio

≥98% (HPLC)

Forma fisica

powder

Colore

white to beige

Solubilità

DMSO: 20 mg/mL, clear

Temperatura di conservazione

2-8°C

Stringa SMILE

O=C1NN=C(CC2=CC=C(F)C(C(N3CCC(OC)CC3)=O)=C2)C4=CC=CC=C41

InChI

1S/C22H22FN3O3/c1-29-15-8-10-26(11-9-15)22(28)18-12-14(6-7-19(18)23)13-20-16-4-2-3-5-17(16)21(27)25-24-20/h2-7,12,15H,8-11,13H2,1H3,(H,25,27)
HYNBNUYQTQIHJK-UHFFFAOYSA-N

Azioni biochim/fisiol

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.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Certificati d'analisi (COA)

Cerca il Certificati d'analisi (COA) digitando il numero di lotto/batch corrispondente. I numeri di lotto o di batch sono stampati sull'etichetta dei prodotti dopo la parola ‘Lotto’ o ‘Batch’.

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MC2050 hydrate ≥98% (HPLC)

Sigma-Aldrich

SML0213

MC2050 hydrate

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Sigma-Aldrich

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PDD00017273

BGP-15 ≥98% (HPLC)

Sigma-Aldrich

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Sigma-Aldrich

Sigma-Aldrich

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Sigma-Aldrich

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BAY 60-2770 ≥98% (HPLC)

Sigma-Aldrich

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Linda Henneman et al.
Proceedings of the National Academy of Sciences of the United States of America, 112(27), 8409-8414 (2015-06-24)
Metaplastic breast carcinoma (MBC) is a rare histological breast cancer subtype characterized by mesenchymal elements and poor clinical outcome. A large fraction of MBCs harbor defects in breast cancer 1 (BRCA1). As BRCA1 deficiency sensitizes tumors to DNA cross-linking agents
Lenka Oplustil O'Connor et al.
Cancer research, 76(20), 6084-6094 (2016-08-24)
The PARP inhibitor AZD2461 was developed as a next-generation agent following olaparib, the first PARP inhibitor approved for cancer therapy. In BRCA1-deficient mouse models, olaparib resistance predominantly involves overexpression of P-glycoprotein, so AZD2461 was developed as a poor substrate for
Józefa Węsierska-Gądek et al.
Journal of cancer prevention, 19(2), 125-136 (2014-10-23)
Cells harboring BRCA1/BRCA2 mutations are hypersensitive to inhibition of poly(ADP-ribose) polymerase-1 (PARP-1). We recently showed that interference with PARP-1 activity by NU1025 is strongly cytotoxic for BRCA1-positive BT-20 cells but not BRCA1-deficient SKBr-3 cells. These unexpected observations prompted speculation that
Knut H Lauritzen et al.
eLife, 10 (2021-08-04)
Poly(ADP-ribose) polymerase (PARP) enzymes initiate (mt)DNA repair mechanisms and use nicotinamide adenine dinucleotide (NAD+) as energy source. Prolonged PARP activity can drain cellular NAD+ reserves, leading to de-regulation of important molecular processes. Here, we provide evidence of a pathophysiological mechanism

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