オラパリブ

化学名:オラパリブ

CAS番号.763113-22-0

英語名:Olaparib

CBNumberCB02473811

MFC24H23FN4O3

MW434.46

MOL File763113-22-0.mol

别名

オラパリブ

オラパリブ (JAN)

4-[[3-[[4-(シクロプロピルカルボニル)-1-ピペラジニル]カルボニル]-4-フルオロフェニル]メチル]-1(2H)-フタラジノン

オラパリブ物理性質

比重(密度)	1.43
貯蔵温度	-20°C
溶解性	DMSO (最大 33mg/ml) またはエタノール (最大 1.7mg/ml) に可溶
酸解離定数(Pka)	12.07±0.40(Predicted)
外見	個体
色	オフホワイト
安定性：	DMSO溶液またはエタノール溶液で-20°Cで最大1か月保存できます。
InChIKey	FDLYAMZZIXQODN-UHFFFAOYSA-N
SMILES	C1(=O)C2=C(C=CC=C2)C(CC2=CC=C(F)C(C(N3CCN(C(C4CC4)=O)CC3)=O)=C2)=NN1
CAS データベース	763113-22-0

安全性情報

Rフレーズ	22-38-37-36
Sフレーズ	24/25-37/39
国連危険物分類	IRRITANT
HSコード	29339900

危険有害性情報のコード(GHS)

オラパリブ化学特性,用途語,生産方法

効能
抗悪性腫瘍薬, PARP阻害薬
商品名
リムパーザ (アストラゼネカ)
説明
Olaparib, marketed by AstraZeneca under the brand name Lynparza , was approved in the USA in December 2014 as a targeted, single-agent therapy for the treatment of germline BRCA-mediated advanced ovarian cancer.Olaparib, originally developed by KuDOS pharmaceuticals and later by AstraZeneca, functions as a poly ADP ribose polymerase inhibitor and has been specifically approved for patients who have received three or more treatments of chemotherapy. In clinical trials, the drug prolonged progression- free survival for patients suffering from platinum-sensitive recurrent serous ovarian cancer. Olaparib is also currently in various phases of investigation for treatment of breast, gastric, prostate, pancreatic and non-small cell lung cancer.
化学的特性
White Solid
使用
Olaparib is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Olaparib has been shown to induce significant killing of ATM-deficient lymphoid tumor cells in vitro and in vivo. Recent studies show that Olaparib increases radiosensitivity of a lung tumor xenograft, making it a potential candidate for use in combination with radiotherapy.
定義
ChEBI: Olaparib is a member of the class of N-acylpiperazines obtained by formal condensation of the carboxy group of 2-fluoro-5-[(4-oxo-3,4-dihydrophthalazin-1-yl)methyl]benzoic acid with the free amino group of N-(cyclpropylcarbonyl)piperazine; used to treat advanced ovarian cancer. It has a role as an antineoplastic agent, an EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor and an apoptosis inducer. It is a N-acylpiperazine, a member of cyclopropanes, a member of monofluorobenzenes and a member of phthalazines.
生物活性
Many of the products generated by alkylating agents on DNA can be efficiently repaired by normal base excision repair (BER). Some poly(ADP-ribose) polymerases (PARPs) assist in the repair of single-strand DNA nicks, an important step in BER. Olaparib is a potent inhibitor of PARP1 and PARP2 (IC50 = 5 and 1 nM, respectively) but is less effective against the PARP tankyrase-1 (IC50 = 1.5 μM). It can be used in cells and in animals, alone or in combination therapy with alkylating agents, to block BER and increase cancer cell death.[Cayman Chemical]
Mode of action
Olaparib is a small molecule inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential chemosensitizing, radiosensitizing, and antineoplastic activities. Olaparib selectively binds to and inhibits PARP, inhibiting PARP-mediated repair of single strand DNA breaks; PARP inhibition may enhance the cytotoxicity of DNA-damaging agents and may reverse tumor cell chemoresistance and radioresistance. PARP catalyzes post-translational ADP-ribosylation of nuclear proteins and can be activated by single-stranded DNA breaks.

オラパリブ生産企業

オラパリブスペクトルデータ(¹HNMR)

763113-22-0, オラパリブキーワード

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オラパリブ

危険有害性情報のコード(GHS)

オラパリブ 化学特性,用途語,生産方法

オラパリブ 生産企業

オラパリブ スペクトルデータ(1HNMR)

763113-22-0, オラパリブ キーワード

オラパリブ化学特性,用途語,生産方法

オラパリブ生産企業

オラパリブスペクトルデータ(¹HNMR)

763113-22-0, オラパリブキーワード