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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 | C26H36N6O |
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分子量 | 448.60 | CAS No. | 1619903-54-6 | |
Solubility (25°C)* | 体外 | Ethanol | 42 mg/mL (93.62 mM) | |
DMSO | 23 mg/mL (51.27 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 | LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9(IC50=0.011 μM) and also inhibits other transcription kinases CDK8(IC50=0.016 μM) and CDK7 (IC50=0.246 μM). |
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in vitro | LY2857785 shows good selectivity against a panel of 114 protein kinases, with only 5 other protein kinases inhibited with potency (IC50) less than 0.1 μmol/L, and a total of 14 kinases less than 1 μmol/L. At the cellular level, LY2857785 inhibits CTD P-Ser2 and CTD P-Ser5 in U2OS cells at IC50s 0.089 and 0.042 μM. Although LY2857785 inhibits CDK4, CDK6, and CDK2 enzymatic activities, it does not induce G1-S cell-cycle arrest. It also has activity against CDK1 (Histone H1 P-T153 inhibition IC50 0.241 μmol/L). However LY2857785 only induces a moderate G2–M DNA content increase, from 35% to 55%, with EC50 0.135 μmol/L. LY2857785 inhibits hematologic and solid tumor cell proliferation and induces apoptosis in vitro[1]. |
in vivo | LY2857785 inhibits RNAP II CTD Ser2 phosphorylation in vivo. It demonstrates potent antitumor growth efficacy in preclinical tumor models and increases animal survival. No significant weight loss is observed in the nude mouse study while animal mortality is observed in these studies at LY2957785 high-dose groups[1]. |
細胞アッセイ | 細胞株 | Solid tumor cells/hematologic cell lines; i.e. Human A549 (lung carcinoma), U2OS (osteosarcoma), HCT116 (colorectal carcinoma), U87MG (glioblastoma), A375 (malignant melanoma), MV-4-11 (biphenotypic B-myelomonocytic leukemia), RPMI 8226 (myeloma), L363 (multiple myeloma) cancer cell lines |
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濃度 | 0, 0.1, 0.2, 0.4, 0.6, 0.8, 1 μM | |
反応時間 | 2-72 h | |
実験の流れ | Solid tumor cells are plated in poly-d-lysine coated and hematologic cell lines are seeded in noncoated 96-well plates overnight before being treated with compounds. Solid tumor cells are fixed with Prefer for 20 minutes at room temperature and permeated with 0.1% Triton X-100 in PBS for 15 minutes. Caspase-3 expression is measured by immunofluorescence with antiactivated caspase-3. Terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL) activity is measured. Hematologic tumor cells are assayed for cell viability. | |
動物実験 | 動物モデル | female nude rats or athymic nude female mice |
投薬量 | 4, 8, 12 mg/kg | |
投与方法 | i.v. |
ChemR23 activation reprograms macrophages toward a less inflammatory phenotype and dampens carcinoma progression [ Front Immunol, 2023, 14:1196731] | PubMed: 37539056 |
Inhibitors Targeting CDK9 Show High Efficacy against Osimertinib and AMG510 Resistant Lung Adenocarcinoma Cells [ Cancers (Basel), 2021, 13(15)3906] | PubMed: 34359807 |
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。