ニラパリブ化学構造式

ニラパリブ

化学名:ニラパリブ

CAS番号.1038915-60-4

英語名:Niraparib

CBNumberCB82514860

MFC19H20N4O

MW320.39

MOL File1038915-60-4.mol

别名

ニラパリブ

2-[4-[(3S)-ピペリジン-3α-イル]フェニル]-2H-インダゾール-7-カルボアミド

2-{4-[(3S)-ピペリジン-3-イル]フェニル}-2H-インダゾール-7-カルボキサミド

ニラパリブ物理性質

融点	187-189°C
沸点	463.6±45.0 °C(Predicted)
比重(密度)	1.34
貯蔵温度	2-8°C(protect from light)
溶解性	DMSO（微量）、メタノール（微量）
酸解離定数(Pka)	15.36±0.30(Predicted)
外見	個体
色	淡黄色～淡黄色

危険有害性情報のコード(GHS)

ニラパリブ化学特性,用途語,生産方法

効能
抗悪性腫瘍薬, PARP阻害薬
説明
(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide is also known as MK-4827(Niraparib) tosylate is a selective inhibitor of PARP1/PARP2 (The poly(ADP-ribose) polymerase) with great activity in cancer cells with mutant BRCA-1 and BRCA-2. It has been recently approved by FDA for the maintenance treatment of adult patients with recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in complete or partial response to platinum-based chemotherapy. In vitro studies have shown that niraparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes resulting in DNA damage, apoptosis and cell death.
使用
Niraparib is a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.
薬理学
The synthesis and initial pharmacology of niraparib have been published. Niraparib has affinity for PARP 1 and 2 inhibition (IC50 = 3.8 and 2.1 nM, respectively) and inhibits the proliferation of cancer cells with mutant BRCA1 and BRCA2 with IC50 values in the 10–100 nM range in vitro. Niraparib demonstrated efficacy as a single agent in a xenograft model of BRCA1-deficient cancer. Niraparib has also been reported to act as a preclinical radiosensitiser and has entered into clinical oncology trials.
参考文献
https://newdrugapprovals.org/2016/12/22/niraparib-mk-4827/
https://www.fda.gov/drugs/informationondrugs/approveddrugs/ucm548487.htm
https://www.drugbank.ca/drugs/DB11793
Sandhu, Shahneen K, et al. "The poly (ADP-ribose) polymerase inhibitor niraparib (MK4827) in BRCA, mutation carriers and patients with sporadic cancer: a phase 1 dose-escalation trial." Lancet Oncology14.9 (2013):882.
Jones, P, et al. "Niraparib: A Poly (ADP-ribose) Polymerase (PARP) Inhibitor for the Treatment of Tumors with Defective Homologous Recombination. " Journal of Medicinal Chemistry 58.8(2015):3302-14.

ニラパリブ上流と下流の製品情報

ニラパリブ生産企業

ニラパリブスペクトルデータ(¹HNMR)

1038915-60-4, ニラパリブキーワード

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ニラパリブ

危険有害性情報のコード(GHS)

ニラパリブ 化学特性,用途語,生産方法

ニラパリブ 上流と下流の製品情報

ニラパリブ 生産企業

ニラパリブ スペクトルデータ(1HNMR)

1038915-60-4, ニラパリブ キーワード

ニラパリブ化学特性,用途語,生産方法

ニラパリブ上流と下流の製品情報

ニラパリブ生産企業

ニラパリブスペクトルデータ(¹HNMR)

1038915-60-4, ニラパリブキーワード