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Merck
所有图片(1)

文件

SML1858

Sigma-Aldrich

AZD2461

≥98% (HPLC)

别名:

4-[4-氟-3-[（4-甲氧基哌啶-1-基）羰基] 苄基] 酞嗪-1 (2H)-酮, 4-[[4-氟-3-[（4-甲氧基-1-哌啶基）羰基] 苯基] 甲基]-1 (2H)-酞嗪酮, 氮杂环-2461, 氮杂环丁烷 (AZD) 2461

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About This Item

经验公式（希尔记法）:
C22H22FN3O3
CAS号:
1174043-16-3
分子量:
395.43
MDL號碼:
MFCD24386811
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

100

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 20 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

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)

InChI 密鑰

HYNBNUYQTQIHJK-UHFFFAOYSA-N

生化／生理作用

AZD2461 是一种奥拉帕尼类似物，这是一种口服、强效、选择性 PARP1 和 PARP2 抑制剂，是药物转运蛋白的弱底物。AZD2461 在过表达 P-糖蛋白的奥拉帕尼耐药肿瘤中表现出了较高的疗效。

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

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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
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
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
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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