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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C33H34N4O4S |
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分子量 | 582.71 | CAS No. | 881375-00-4 | |
Solubility (25°C)* | 体外 | DMSO | 2 mg/mL (3.43 mM) | |
Water | Insoluble | |||
Ethanol | 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 | KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC50 of 0.59 μM. |
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in vitro | KU-0060648 exhibits differential effects on growth inhibition, but is not profoundly cytotoxic in a panel of human cancer cell lines. It inhibits DNA-PK and PI-3K with greater potency in MCF7 than SW620 cell using cell-based assays. Five-day exposure to 1 mM KU-0060648 inhibits cell proliferation by more than 95% in MCF7 cells but only by 55% in SW620 cells. In clonogenic survival assays, KU-0060648 increases the cytotoxicity of etoposide and doxorubicin across the panel of DNA-PKcs-proficient cells, but not in DNA-PKcs-deficient cells, confirming that enhanced cytotoxicity of the topoisomerase II poisons etoposide and doxorubicin is due to DNA-PK inhibition. [1] |
in vivo | KU-0060648 enhances the anti-tumour activity of etoposide in both MCF7 and SW620 xenograft models, and has single-agent activity in the MCF7 xenograft model. [1] |
細胞アッセイ | 細胞株 | MCF7, T47D, MDA-MB-231, LoVo and SW620 |
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濃度 | ~1 μM | |
反応時間 | 5 day | |
実験の流れ | SRB assay | |
動物実験 | 動物モデル | human-tumor SW620 or MCF7 xenograft models |
投薬量 | 10 mg/kg, twice daily | |
投与方法 | i.p. |
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Data from [Data independently produced by , , Genome Med, 2015, 7:93]
Data from [Data independently produced by , , Mol Cancer Ther, 2018, 17(2): 419-31]
Combined inhibition of EZH2 and ATM is synthetic lethal in BRCA1-deficient breast cancer [ Breast Cancer Res, 2022, 24(1):41] | PubMed: 35715861 |
Identifying Novel Actionable Targets in Colon Cancer [ Biomedicines, 2021, 9(5)579] | PubMed: 34065438 |
Development of a CRISPR-Cas9 Based Luciferase Turn-On System as Nonhomologous End Joining Pathway Reporter [ Chembiochem, 2021, 22(12):2177-2181] | PubMed: 33882189 |
UBQLN4 Represses Homologous Recombination and Is Overexpressed in Aggressive Tumors [Jachimowicz RD, et al Cell, 2019, 176(3):505-519] | PubMed: 30612738 |
Temozolomide Induces Senescence and Repression of DNA Repair Pathways in Glioblastoma Cells via Activation of ATR-CHK1, p21, and NF-κB [ Cancer Res, 2019, 79(1):99-113] | PubMed: 30361254 |
Curcumin sensitizes lymphoma cells to DNA damage agents through regulating Rad51-dependent homologous recombination [Zhao Q, et al. Biomed Pharmacother, 2018, 97:115-119] | PubMed: 29080451 |
Modeling chemotherapy-induced stress to identify rational combination therapies in the DNA damage response pathway [ Sci Signal, 2018, 11(540)eaat0229] | PubMed: 30042127 |
A CRISPR/Cas9-Based Screening for Non-Homologous End Joining Inhibitors Reveals Ouabain and Penfluridol as Radiosensitizers [Du J, et al. Mol Cancer Ther, 2018, 17(2):419-431] | PubMed: 28864683 |
Targeting Homologous Recombination by Pharmacological Inhibitors Enhances the Killing Response of Glioblastoma Cells Treated with Alkylating Drugs. [ Mol Cancer Ther, 2016, 15(11):2665-2678] | PubMed: 27474153 |
Artesunate enhances the therapeutic response of glioma cells to temozolomide by inhibition of homologous recombination and senescence. [Berte N, et al. Oncotarget, 2016, 7(41):67235-67250] | PubMed: 27626497 |
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。