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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C15H15FN6O2S2 |
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分子量 | 394.45 | CAS No. | 1421693-22-2 | |
Solubility (25°C)* | 体外 | DMSO | 79 mg/mL (200.27 mM) | |
Ethanol | 1.5 mg/mL (3.8 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 | CDKI-73 (LS-007) is a potent CDK inhibitor in vitro with IC50 of 8.17 nM, 3.27 nM, 8.18 nM, and 5.78 nM for CDK1, CDK2, CDK4, and CDK9, respectively. CDKI-73 induces apoptosis in cancer cells. CDKI-73 is an orally bioavailable and highly efficacious CDK9 inhibitor against acute myeloid leukemia. |
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in vitro | CDKI-73 induces cancer cells undergoing apoptosis through transcriptional downregulation of anti-apoptotic proteins Bcl-2, Mcl-1 and XIAP by majorly targeting CDK9. Contrastively, it is relatively low toxic to the bone marrow cells of healthy donors.[2] |
in vivo | CDKI-73 is orally bioavailable, highly efficacious against MLL-AML MV4–11 xenografts and downregulates anti-apoptotic proteins by targeting CDK9 in vivo.[2] |
細胞アッセイ | 細胞株 | Leukemia cell lines (MOLM13, MV4-11, THP-1, etc.) |
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濃度 | 0.05 μM, 0.1 μM, 0.25 μM, 0.5 μM | |
反応時間 | 1 h, 4 h, 12 h, 24 h, 48 h | |
実験の流れ | MV4-11 (1 × 105/well) cells are seeded and incubated under 5% CO2 at 37ºC overnight. After incubation with indicated concentrations of the CDKI-73 for 24 or 48 h, cells are collected and centrifuged (300 g, 5 min). For cell cycle assay, the pellets are re-suspended in cold 70% ethanol and fixed on ice for 15 min, followed by centrifugation (300 g, 5 min). The collected pellets are incubated with 200 μL staining solution at 37ºC for 1 h, then analyzed with a Gallios flow cytometer. Apoptosis is assessed with cells collected and processed as per the instruction in the annexin V-FITC/PI commercial kit. |
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動物実験 | 動物モデル | female nude (nu/nu) Balb/C mice aged 6–8 weeks |
投薬量 | 25 mg/kg | |
投与方法 | Oral gavage |
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pH-Responsive Poly(ethylene glycol)-b-poly(2-vinylpyridine) Micelles for the Triggered Release of Therapeutics [ Pharmaceutics, 2023, 15(3)977] | PubMed: 36986838 |
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。