Saruparib (AZD5305)

製品コードS9875 バッチS987501

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C22H26N6O2
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
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.

溶剤液（一定の濃度）を調合する

生物活性

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).
in vitro

Saruparib (AZD5305) is a highly selective inhibitor for PARP1 over other PARP family members, with good secondary pharmacology and physicochemical properties and excellent pharmacokinetics in preclinical species. It reduces anti-proliferation effects on human bone marrow progenitor cells in vitro.

[2]
in vivo

Saruparib (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.[2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 DLD-1 cells, BRCA2 (-/-) DLD-1 cells
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. Saruparib (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. 
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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/34904816/
  • https://pubmed.ncbi.nlm.nih.gov/34570508/
  • https://pubmed.ncbi.nlm.nih.gov/35929986/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Transcription-replication conflicts underlie sensitivity to PARP inhibitors [ Nature, 2024, 10.1038/s41586-024-07217-2] PubMed: 38509368
Transcription-replication conflicts underlie sensitivity to PARP inhibitors [ Nature, 2024, 628(8007):433-441] PubMed: 38509368
PARG is essential for Polθ-mediated DNA end-joining by removing repressive poly-ADP-ribose marks [ Nat Commun, 2024, 15(1):5822] PubMed: 38987289
PARP inhibitors suppress tumours via centrosome error-induced senescence independent of DNA damage response [ EBioMedicine, 2024, 103:105129] PubMed: 38640836
CHD1L Regulates Cell Survival in Breast Cancer and Its Inhibition by OTI-611 Impedes the DNA Damage Response and Induces PARthanatos [ Int J Mol Sci, 2024, 25(16)8590] PubMed: 39201277

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。

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