【PARP抑制劑-Olaparib】Potent PARP1/PARP2 inhibitor-CAS#763113-22-0 Apexbio
雷帕黴菌（Rapamycin）| Romidepsin (FK228, depsipeptide) | Daptomycin | G-418 (80 S 核醣體延伸抑制劑)
奧拉帕尼(Olaparib (AZD2281, Ku-0059436)| CAS#763113-22-0 APExBIO 貨號 A4154
Potent PARP1/PARP2 inhibitor
Olaparib (4-(3-4-fluorophenyl) methyl-1(2H)-one)，稱為 AZD2281 或 KU0059436，是一種新型、選擇性和有效的抑製劑，可抑制聚腺苷二磷酸-核糖多聚體-1 (poly adenosine diphosphate-ribose polymeras-1 , PARP-1) ) 和聚腺苷二磷酸-核糖多聚體-2 (poly adenosine diphosphate-ribose polymeras-2, PARP-2)。奧拉帕尼(Olaparib)已成功用於治療攜帶 BRCA 突變的腫瘤，可強烈抑制 BRCA2 缺陷小鼠二元腫瘤細胞系的生長，表現出細胞毒性。在之前治療非小細胞肺癌 (non-small cell lung carcinoma , NSCLC) 的研究中，奧拉帕尼(Olaparib)增加了 NSCLC 細胞的輻射敏感性，這些細胞在輻射後在裸鼠中作為異種移植物生長，並增加了dorsal window chamber (dorsal window chamber , DWC) 中建立的 Calu-6 腫瘤中的vascular perfusion。
| Storage | Store at -20°C |
| M.Wt | 434.46 |
| Cas No. | 763113-22-0 |
| Formula | C24H23FN4O3 |
| Synonyms | AZD 2281,AZD-2281 |
| Solubility | ≥21.72 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| Chemical Name | 4-[[3-[4-(cyclopropanecarbonyl)piperazine-1-carbonyl]-4-fluorophenyl]methyl]-2H-phthalazin-1-one |
| SDF | Download SDF |
| Canonical SMILES | C1CC1C(=O)N2CCN(CC2)C(=O)C3=C(C=CC(=C3)CC4=NNC(=O)C5=CC=CC=C54)F |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon. |
1. Leonie Schürmann, Lena Schumacher, et al. “Inhibition of the DSB repair protein RAD51 potentiates the cytotoxic efficacy of doxorubicin via promoting apoptosis-related death pathways.” Cancer Lett. 2021 Nov 1;520:361-373. PMID:34389435
2. Asha Sinha, Sachin Katyal, et al. “PARP-DNA trapping ability of PARP inhibitors jeopardizes astrocyte viability: Implications for CNS disease therapeutics.” Neuropharmacology. 2021 Apr 1;187:108502. PMID:33631119
3. Phoebe McCrorie, Jatin Mistry, et al. “Etoposide and olaparib polymer-coated nanoparticles within a bioadhesive sprayable hydrogel for post-surgical localised delivery to brain tumours.” Eur J Pharm Biopharm. 2020 Oct 14;S0939-6411(20)30305-2. PMID:33068736
4. Kim DS, Camacho CV, et al. “Activation of PARP-1 by snoRNAs Controls Ribosome Biogenesis and Cell Growth via the RNA Helicase DDX21.” Mol Cell. 2019 Jul 9. pii: S1097-2765(19)30476-9. PMID:31351877
5. Singatulina AS, Hamon L, et al. “PARP-1 Activation Directs FUS to DNA Damage Sites to Form PARG-Reversible Compartments Enriched in Damaged DNA.” Cell Rep. 2019 May 7;27(6):1809-1821.e5. PMID:31067465
6. Kong X, Cruz GMS, et al. “Biphasic recruitment of TRF2 to DNA damage sites promotes non-sister chromatid homologous recombination repair.” J Cell Sci. 2018 Dec 5;131(23). pii: jcs219311. PMID:30404833
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APExBIO提供優質的胜肽和生物分析試劑，廣泛產品線如Protease、Chromatin/Epigenetics表觀遺傳學、MAPK Signal、DNA Damege/DNA repair、細胞凋亡、腫瘤生物學、Stem cell等研究領域， 還提供定制的服務，包括多肽合成，抗體的生產和檢測的發展。產品線DNA/RNA prep kit、Drug Screening panel、Bioactive peptides、Growth factors、Biotinylation Reagents、tag peptides、amino Acids、Growth factors等。APExBIO產品質量都伴隨著證書的分析，高效液相色譜，質譜，和HMNR數據。
| APExBIO產品線 | 品項 | CAS# | #貨號 |
| Proteases | Z-VAD-FMK | CAS# 187389-52-2 APExBIO | CAS# 187389-52-2 | 貨號 A1902 |
| Proteinase K | 蛋白酶 K (Proteinase K) | CAS#39450-01-6 APExBIO 貨號K1037 | CAS#39450-01-6 | 貨號K1037 |
| 品項 | CAS# | #貨號 | 應用 |
| Romidepsin (FK228, depsipeptide) |
CAS#128517-07-7
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貨號A8173 | HDAC1/HDAC2，強效和選擇性抑制劑 |
| Pirarubicin | CAS#72496-41-4 | 貨號B2295 | anthracycline anti-neoplastic doxorubicin |
| Tunicamycin | CAS# 15663-27-1 |
貨號A8321
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高效、廣譜的化療藥物 |
| Azithromycin | CAS#83905-01-5 | 貨號A2213 | Hsp90 inhibitor |
| Bleomycin Sulfate |
CAS# 9041-93-4
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貨號B1398 | Antibiotic by inhibiting protein synthesis |
| Nystatin (Fungicidin) | CAS#1400-61-9 | 貨號B1993 | antifungal antibiotic |
| Rapamycin | CAS#53123-88-9 | 貨號A8167 | Original antifungal antibiotic |
| Daptomycin | CAS#103060-53-3 | 貨號A1206 | Calcium-dependent antibiotic |
| 品項 | CAS# | #貨號 | 應用 |
| Z-VAD-FMK | CAS# 187389-52-2 | 貨號 A1902 |
Proteases ICE-like proteases |
| TAPI-1 | CAS#171235-71-5 | 貨號 B4686 |
Proteases TACE/ADAM17 inhibitor Product Citation+3 |
| Talabostat mesylate | CAS# 150080-09-4 | 貨號B3941 |
Proteases DPP4 二肽基肽酶特異性抑制劑 |
| Z-IETD-FMK | CAS# 210344-98-2 | 貨號B3232 | inhibitor of caspase 8 |
| Cisplatin | CAS# 15663-27-1 | 貨號A8321 | 高效、廣譜的化療藥物 |
| 17-DMAG (Alvespimycin) HCl | CAS#467214-21-7 | 貨號A2213 | Hsp90 inhibitor |
| CA-074 Me | CAS# 147859-80-1 | 貨號A8239 | Cathepsin B inhibitor |
| VX-765 | CAS# 273404-37-8 | 貨號A8238 | Caspase-1 inhibitor |