受注:045-509-1970 |
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Synonyms | CCT0129397 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C19H18ClN3O4 |
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分子量 | 387.82 | CAS No. | 940289-57-6 | |
Solubility (25°C)* | 体外 | DMSO | 77 mg/mL (198.54 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 | VER-49009 (CCT0129397) is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β. |
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in vitro | VER-49009 inhibits the intrinsic ATPase activity of recombinant yeast Hsp90 with IC50 of 167 nM, and produces antiproliferative activity in a panel of human cancer cell lines and nontumorigenic cells in vitro. VER-49009 causes induction of HSP72 and HSP27 with depletion of client proteins, including C-RAF, B-RAF, and survivin, and PRMT5, which further result in cell cycle arrest and apoptosis. [1] VER-49009 inhibits the cell proliferation, and induces G2 phase arrest in hepatic stellate cell line CFSC cells, which may suggest a rational approach in the prevention of liver fibrosis. [2] |
in vivo | In athymic mice, VER-49009 (20 mg/kg, i.v.) shows rapid clearance with values of 0.187 L/h. In an orthotopic human ovarian carcinoma model, VER-49009 (4 mg/kg, i.p.) also induces the depletion of the sensitive HSP90 client protein ERBB2. [1] |
キナーゼアッセイ | Fluorescence Polarization Assay | |
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Binding of HSP90 inhibitors to human full-length recombinant HSP90β is determined by a competitive binding fluorescence polarization assay, using a fluorescent pyrazole resorcinol probe. | ||
細胞アッセイ | 細胞株 | Melanoma cells (SKMEL 2, SKMEL 5, SKMEL 28, WM266.4); Colon cancer cells (HCT116, BEneg, BE2, HT29, HT29oxaliR); Ovarian cancer cells (CH1, CH1doxR); Breast cancer cells (MB-231, MB-468, BT20, ZR751, MCF7, BT-474); nontumorigenic cells (HUVEC, MCF10a, PNT |
濃度 | ~10 μM | |
反応時間 | 4 days | |
実験の流れ | Antiproliferative effects are measured using the sulforhodamine B assay. HUVEC sensitivity is determined by an alkaline phosphatase method. |
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動物実験 | 動物モデル | Mice bearing established OVCAR3 human ovarian xenografts. |
投薬量 | ~4 mg/kg | |
投与方法 | i.p. |
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deepOrganoid: A brightfield cell viability model for screening matrix-embedded organoids [ SLAS Discov, 2022, 27(3):175-184] | PubMed: 35314378 |
Evolution of kinase polypharmacology across HSP90 drug discovery [ Cell Chem Biol, 2021, S2451-9456(21)00221-X] | PubMed: 34077750 |
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。