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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C22H26N6O2 |
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分子量 | 406.48 | CAS No. | 2589531-76-8 | |
Solubility (25°C)* | 体外 | DMSO | 20 mg/mL (49.2 mM) | |
Ethanol | 2 mg/mL (4.92 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Saruparib (AZD5305) is a highly selective and potent inhibitor of PARP1 with an IC50 of 3 nM in wild-type A549 lung cancer cells. AZD5305 shows no or minimal growth inhibitory effects in other cells (IC50s >10μM). |
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in vitro | AZD5305 is highly selective inhibitor for PARP1 over other PARP family members, with good secondary pharmacology and physicochemical properties and excellent pharmacokinetics in preclinical species. AZD5305 reduces anti-proliferation effects on human bone marrow progenitor cells in vitro. |
in vivo | AZD5305 is a potent and selective PARP1 inhibitor and PARP1–DNA trapper with excellent in vivo efficacy in a BRCA mutant HBCx-17 PDX model.<sup><a class="sref" href="#s_ref">[2]</a></sup> |
細胞アッセイ | 細胞株 | DLD-1 cells, BRCA2 (-/-) DLD-1 cells |
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濃度 | 0.0001-10 μM | |
反応時間 | 7 days | |
実験の流れ | DLD-1 and BRCA2(-/-) DLD-1 cells are harvested to a density of 5000 cells/mL and 2.5 × 104 cells/mL, respectively, in complete media, 40 μL/well seeded into 384-well plates using a Multidrop Combi then incubated at 37 °C, 5% CO2 overnight. The next day (day 1) using a Multidrop Combi, sytox green (5 μL, 2 μM) and saponin (10 μL, 0.25% stock) to a day 0 plate are added, the plate is sealed using a black adhesive lid and incubated for >3 h at rt. Cells are imaged using Cell Insight fitted with a 4× objective. AZD5305 is added using an Echo 555 and placed in an incubator maintained at 37 °C, 5% CO2 and incubated for 7 days. On day 8, sytox green (5 μL, 2 μM) and then saponin (10 μL, 0.25% stock) is added to plates, the plate is sealed using a black adhesive lid and incubated for >3 h at rt. All cells are read on a Cell Insight with 4× Objective. |
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動物実験 | 動物モデル | mouse, rat, dog, cynomolgus monkey |
投薬量 | 10, 1, 0.1, and 0.03 mg/kg | |
投与方法 | p.o. |
Transcription-replication conflicts underlie sensitivity to PARP inhibitors [ Nature, 2024, 10.1038/s41586-024-07217-2] | PubMed: 38509368 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。