올라파립

올라파립 속성

올라파립 C화학적 특성, 용도, 생산

개요

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.

화학적 성질

White Solid

용도

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.

정의

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.

생물학적 활성

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.

올라파립 준비 용품 및 원자재

원자재

준비 용품

올라파립 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Huadong Medicine (Xi'an)Bodyguard Pharmaceutical Co.,Ltd.	+86-029-86185165 +8618629664246	guoyuan@eastchinapharm.com	China	1615	58
Zhengzhou Anhuida Chemical Co., Ltd	+8615903659408	admin@ahdchem.com	China	298	58
Jewim Pharmaceutical (Shandong) Co., Ltd.	+86-15552509998 +86-15621883869	liutf@jewim.com.cn	China	251	58
Seasons Biotechnology Co., Ltd.	+86-0576-89232655 +86-13566878689	info@seasonsbio.com	China	46	58
Hefei TianRui Pharmaceutical Chemical Co., Ltd.	+86-0551-68665055 +86-+86-18616906106	sales@trywchem.com	China	129	58
Guangzhou Tosun Pharmaceutical Limited	+8618922120635	sales@toref-standards.com	China	1000	58
Wuhan Quanjinci New Material Co.,Ltd.	+8615271838296	kyra@quanjinci.com	China	1532	58
Zibo Hangyu Biotechnology Development Co., Ltd	+86-0533-2185556 +8617865335152	Mandy@hangyubiotech.com	China	11013	58
SHANDONG BOYUAN PHARMACEUTICAL CO., LTD.	+86-0531-69954981 +8615666777973	dwyane.wang@boyuanpharm.com	China	211	58
Hebei Yanxi Chemical Co., Ltd.	+8617531190177	peter@yan-xi.com	China	5993	58

올라파립 관련 검색: