货号:A134565 同义名: AZD2281;KU0059436
Olaparib 是一种 PARP 抑制剂,对 PARP1 和 PARP2 具有高亲和力,IC50 值分别为 5 nM 和 1 nM。Olaparib 具有抗肿瘤作用,可用于 BRCA 突变相关癌症的研究。
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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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产品名称 | PARP ↓ ↑ | PARP1 ↓ ↑ | PARP2 ↓ ↑ | PARP3 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
PJ34 HCl |
++
PARP, EC50: 20 nM |
99%+ | |||||||||||||||||
Rucaparib phosphate |
++++
PARP, Ki: 1.4 nM |
99%+ | |||||||||||||||||
3-Aminobenzamide |
++
PARP, IC50: <50 nM |
98% | |||||||||||||||||
AZD-2461 | ✔ | 99%+ | |||||||||||||||||
BGP-15 | ✔ | 99%+ | |||||||||||||||||
NU1025 |
+
PARP, IC50: 400 nM |
97% | |||||||||||||||||
Benzamide |
+
PARP, IC50: 3.3 μM |
98% | |||||||||||||||||
Picolinamide |
+
PARP, IC50: 95 μM |
98% | |||||||||||||||||
AG14361 |
+++
PARP1, Ki: <5 nM |
98+% | |||||||||||||||||
Iniparib | ✔ | 98% | |||||||||||||||||
Talazoparib |
++++
PARP1, IC50: 0.57 nM |
99%+ | |||||||||||||||||
NMS-P118 |
++
PARP1, Kd: 0.009 μM |
98+% | |||||||||||||||||
UPF 1069 |
+
PARP1, IC50: 8.0 μM |
++
PARP2, IC50: 0.3 μM |
98% | ||||||||||||||||
A-966492 |
++++
PARP1, Ki: 1 nM PARP1, EC50: 1 nM |
+++
PARP2, Ki: 1.5 nM |
99%+ | ||||||||||||||||
Veliparib |
++
PARP1, Ki: 5.2 nM |
+++
PARP2, Ki: 2.9 nM |
98% | ||||||||||||||||
Niraparib tosylate |
+++
PARP1, IC50: 3.8 nM |
+++
PARP2, IC50: 2.1 nM |
99%+ | ||||||||||||||||
Stenoparib |
++++
PARP1, IC50: 1 nM |
++++
PARP2, IC50: 1.2 nM |
98% | ||||||||||||||||
Olaparib |
+++
PARP1, IC50: 5 nM |
++++
PARP2, IC50: 1 nM |
98% | ||||||||||||||||
Niraparib |
+++
PARP1, IC50: 3.8 nM |
+++
PARP2, IC50: 2.1 nM |
98% | ||||||||||||||||
ME0328 |
+
PARP1, IC50: 6.3 μM |
+
PARP3, IC50: 0.89 μM |
99%+ | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | PARP1, also called as Poly(ADP-ribose) polymerase, is involved in the signaling of DNA damage. It can recognize and bind DNA single or double-strand breaks . Thus it possesses various cellular function, including regulation of apoptosis and chromosome stability, gene amplification and transcription, as well as cell division and differentiation. PARP-2 is the closest homolog of PARP1 (~62% similarity in catalytic domain) and compensates for PARP-1 activity in DNA single-strand break repair[1]. Olaparib, also called as AZD2281 or Ku-0059436, one of the best investigated third-generation PARP inhibitors[2], can potently inhibit both PARP-1 (IC50=5nM) and PARP-2(IC50=1nM)[1]. BRCA1-deficient cell lines, such as MDA-MB-436 and HCC1937, were hypersensitive to olaparib than BRCA1- and BRCA2-proficient cell lines (Hs578T, MDA-MB-231 and T47D). Also olaparib shows good pharmacokinetic profiles, oral bioavailability, as well as activity in vivo[1]. These facilitate olaparib approved for use in recurrent ovarian cancer and germline BRCA HER2-negative metastatic breast cancer[2]. |
作用机制 | Olaparib occupies the NAD binding pocket at the catalytic site, which has been proposed to trap PARP1 on DNA.[3] |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
5637 | Growth Inhibition Assay | IC50=7.9286 μM | SANGER | ||
697 | Growth Inhibition Assay | IC50=2.84173 μM | SANGER | ||
769-P | Growth Inhibition Assay | IC50=24.8466 μM | SANGER | ||
8505C | Growth Inhibition Assay | IC50=26.4977 μM | SANGER | ||
Dose | Mice: min = 10 mg/kg[4], max = 200 mg/kg[5] |
Administration | p.o., i.v., i.p. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT02571725 | Ovarian Cancer ... 展开 >> Fallopian Tube Cancer Peritoneal Neoplasms 收起 << | Phase 1 Phase 2 | Recruiting | February 2022 | United States, Florida ... 展开 >> Moffitt Cancer Center Recruiting Tampa, Florida, United States, 33612 Contact: Eleni Rokakis, BSN, RN 813-745-3593 Eleni.Rokakis@moffitt.org United States, New Mexico Southwest Gynecologic Oncology Associates Recruiting Albuquerque, New Mexico, United States, 87106 Contact: Karen Finkelstein, MD 505-843-7813 University of New Mexico Comprehensive Cancer Center Recruiting Albuquerque, New Mexico, United States, 87131 Contact: Valerie Parks, RN 505-925-0390 vparks@salud.unm.edu Principal Investigator: Sarah F Adams, MD United States, Ohio The Ohio State University Recruiting Columbus, Ohio, United States, 43210 Contact: David M O'Malley, MD 614-685-6411 Contact: Molly Myers 614-685-6411 molly.myers@osumc.edu United States, Virginia University of Virginia Cancer Center Recruiting Charlottesville, Virginia, United States, 22903 Contact: Anne Gabel 434-982-6657 am7bd@virginia.edu 收起 << |
NCT03579784 | Advanced Gastric Cancer | Phase 2 | Recruiting | April 30, 2020 | Korea, Republic of ... 展开 >> Seoul National University Hospital Recruiting Seoul, Korea, Republic of, 110-744 Contact: Do-Youn Oh, MD, PhD 82-2-2072-0701 ohdoyoun@snu.ac.kr 收起 << |
NCT01972217 | Metastatic Castration-resistan... 展开 >>t Prostate Cancer 收起 << | Phase 2 | Active, not recruiting | December 31, 2018 | - |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.30mL 0.46mL 0.23mL |
11.51mL 2.30mL 1.15mL |
23.02mL 4.60mL 2.30mL |
CAS号 | 763113-22-0 |
分子式 | C24H23FN4O3 |
分子量 | 434.46 |
别名 | AZD2281;KU0059436;Olaparib. trade name Lynparza.;KU59436 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Room temperature |
溶解度 |
DMSO: 105 mg/mL(241.68 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 无水乙醇: 2.5 mg/mL(5.75 mM),配合低频超声,并水浴加热至45℃助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇 DMF: 50 mg/mL(115.08 mM),配合低频超声助溶 |
动物实验配方 |
IP 2% DMSO+2% Tween80+30% PEG300+water 2 mg/mL clear PO 0.5% CMC-Na 45 mg/mL suspension |