Olaparib

Olaparib Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

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.

Chemische Eigenschaften

White Solid

Verwenden

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.

Definition

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.

Biologische Aktivität

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.

Olaparib Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

Olaparib Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
Zhengzhou Anhuida Chemical Co., Ltd	+8615903659408	admin@ahdchem.com	China	286	58
Seasons Biotechnology Co., Ltd.	+86-0576-89232655 +86-13566878689	info@seasonsbio.com	China	47	58
Hefei TianRui Pharmaceutical Chemical Co., Ltd.	+86-0551-68665055 +86-+86-18616906106	sales@trywchem.com	China	148	58
Wuhan Quanjinci New Material Co.,Ltd.	+86-15271838296; +8615271838296	kyra@quanjinci.com	China	1512	58
Zibo Hangyu Biotechnology Development Co., Ltd	+86-0533-2185556 +8615965530500	nickzhang@hangyubiotech.com	China	10985	58
SHANDONG BOYUAN PHARMACEUTICAL CO., LTD.	+86-0531-88625728 +8615165060815	sheldon.chai@boyuanpharm.com	China	183	58
Hebei Mujin Biotechnology Co.,Ltd	+8613288715578	sales@hbmojin.com	China	12628	58
Hebei Yanxi Chemical Co., Ltd.	+8618531123677	faithe@yan-xi.com	China	5853	58
RongNa Biotechnology Co.,Ltd	+86-86-13583358881 +8618560316533	Brad@rongnabiotech.com	China	3064	58
Sinoway Industrial co., ltd.	0592-5800732; +8613806035118	xie@china-sinoway.com	China	1000	58

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• 1-(Cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)Methyl]-2-fluorobenzoyl]piperazin
• Olaparid AZD2281
• 4-(3-(4-(Cyclopropanecarbonyl)piperazine-1-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one
• 4-[[3-[[4-(Cyclopropylcarbonyl)-1-piperazinyl]carbonyl]-4-fluorophenyl]Methyl]-1(2H)-phthalazinone
• KU 59436
• AZD2281(olaparib)/AZD-2281
• AZD2281(olaparib)
• 4-(3-(1-(cyclopropanecarbonyl)piperazine-4-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one
• Olaparib-D8
• Olaparib, 99%, PARP inhibitor
• AZD 2281 - Olaparib | KU 0059436
• AZD2281; KU-0059436; KU0059436; AZD-2281; KU0059436; AZD 2281
• CS-1931
• (937799-91-2) olaparib
• AZD2281,?Ku-0059436
• Olaparib (AZD2281, Ku-0059436)
• Olaparid
• Olaparib 1-(Cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)methyl]-2-fluorobenzoyl]piperazine
• Olaparib, >=98%
• 4-[(3-[(4-cyclopropylcarbonyl)piperazin-4-yl]carbonyl) -4-fluorophenyl]methyl(2H)phthalazin-1-one
• Oraparib
• 1-(Cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)methyl]-2-fluorobenzoyl]pipera
• Azd 2281
• Azd2281
• Azd-2281
• Ku-0059436
• 4-[3-(4-Cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one Olaparib
• 4-[3-(4-Cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one
• Olaparib
• 1-(Cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)methyl]-2-fluorobenzoyl]piperazine
• Olaparib(AZD-2281)
• AZD2281; AZD-2281; AZD 2281; KU59436; KU-59436; KU 59436; KU0059436; KU-0059436; KU 0059436; OLAPARIB. TRADE NAME LYNPARZA.
• Olaparib. trade name Lynparza.
• Olapani
• 1(2H)-Phthalazinone, 4-[[3-[[4-(cyclopropylcarbonyl)-1-piperazinyl]carbonyl]-4-fluorophenyl]methyl]-
• Olaparib USP/EP/BP
• Olaparibr
• Olaparib (API)
• 4-{[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorophenyl]methyl}-1,2-dihydrophthalazin-1-one
• 4-(3-(4-(Cyclopropanecarbonyl)piperazine-1-carbonyl)-4-fluorobenzyl)phthalazine-1(2H)-one
• Mr Parry
• PARP,AZD-2281,Mitochondrial Autophagy,inhibit,Autophagy,orally,KU-0059436,Inhibitor,Olaparib,PARP1,Mitophagy,poly ADP ribose polymerase,KU 0059436,AZD 2281,PARP2
• Olapali
• 4- (3- (4- (cyclopropanecarbonyl) piperazin-1-carbonyl) -4-fluorobenzyl) phthalazin-1 (2H) - one
• Olaparib (Form A)
• 0laparib
• Olaparib Anhydrous Substance
• 4-[[3-[[4-(Cyclopropylcarbonyl)piperazin-1-yl]carbonyl]-4-fluorophenyl]methyl]-1(2H)-phthalazinone
• Olaparib, 10 mM in DMSO
• Olaparib - Bio-X ?
• 763113-22-0
• 63113-22-0
• 763113-22-1
• APIs
• Inhibitors
• Inhibitor
• API
• 763113-22-0