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Synonyms | LEE011 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C23H30N8O |
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分子量 | 434.54 | CAS No. | 1211441-98-3 | |
Solubility (25°C)* | 体外 | DMSO | 20 mg/mL (46.02 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 | Ribociclib is an orally available, and highly specific inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM. Phase 3. |
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in vitro | LEE011, as dual CDK4/CDK6 inhibitor, significantly inhibits the growth of 12 of 17 neuroblastoma cell lines with mean IC50 of 307 nM. The growth inhibition of neuroblastoma cell lines is primarily cytostatic and is mediated by a G1 cell-cycle arrest and cellular senescence. [1] |
in vivo | LEE011 (200 mg/kg daily, p.o.) significantly causes tumor growth delay in mice harboring the BE2C or 1643 xenografts with no weight loss or other signs of toxicity. [1] |
特徴 | Orally bioavailable CDK4/6-selective inhibitor that has been tested in Phase III clinical trials for treatment of advanced breast cancer. |
細胞アッセイ | 細胞株 | BE2C, IMR5, 1643, SY5Y, CHP134, SKNSH, NGP, KELLY, LAN5, NLF, NB69, SKNDZ, NBSD, NBLS, SKNFI, EBC1, SKNAS, NB16, RPE1 cell lines. |
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濃度 | 10 μM | |
反応時間 | ~100 hours | |
実験の流れ | A panel of neuroblastoma cell lines, selected based upon prior demonstration of substrate adherent growth, is plated in triplicate on the Xcelligence Real-Time Cell Electronic Sensing system and treated 24 hours later with a four-log dose range of inhibitor or with a dimethyl sulfoxide (DMSO) control. Cell indexes are monitored continuously for ~100 hours, and IC50 values are determined as follows: growth curves are generated by plotting the cell index as a function of time and are normalized to the cell index at the time of treatment for a baseline cell index of 1. The area under the normalized growth curve from the time of treatment to 96 hours posttreatment is then calculated using a baseline area of 1 (the cell index at the time of treatment). Areas are normalized to the DMSO control, and the resulting data are analyzed using a nonlinear log inhibitor versus normalized response function. All experiments are repeated at least once. |
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動物実験 | 動物モデル | Mice bearing BE2C, NB-1643, or EBC1 xenografts. |
投薬量 | ~200 mg/kg daily | |
投与方法 | p.o. |
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, , Cancer Cell Int, 2017, 17:35
Data from [Data independently produced by , , Nature, 2017, 553(7686):91-95]
Data from [Data independently produced by , , Clin Cancer Res, 2017, 23(22):6958-6968]
Ribociclib leverages phosphodiesterase 4 inhibition in the treatment of neutrophilic inflammation and acute respiratory distress syndrome [ J Adv Res, 2024, S2090-1232(24)00119-X] | PubMed: 38548264 |
Drug Repositioning via Graph Neural Networks: Identifying Novel JAK2 Inhibitors from FDA-Approved Drugs through Molecular Docking and Biological Validation [ Molecules, 2024, 29(6)1363] | PubMed: 38542998 |
The Combination of Afatinib With Dasatinib or Miransertib Results in Synergistic Growth Inhibition of Stomach Cancer Cells [ World J Oncol, 2024, 15(2):192-208] | PubMed: 38545471 |
p21 Prevents the Exhaustion of Cluster of Differentiation 4-Positive T Cells Within the Antitumor Immune Response Against Colorectal Cancer [ Gastroenterology, 2023, S0016-5085(23)05008-4] | PubMed: 37734420 |
Cell facilitation promotes growth and survival under drug pressure in breast cancer [ Nat Commun, 2023, 14(1):3851] | PubMed: 37386030 |
Macrophage inflammatory and regenerative response periodicity is programmed by cell cycle and chromatin state [ Mol Cell, 2023, 83(1):121-138.e7] | PubMed: 36521490 |
N-acetylcysteine overcomes NF1 loss-driven resistance to PI3Kα inhibition in breast cancer [ Cell Rep Med, 2023, 4(4):101002] | PubMed: 37044095 |
New hormone receptor-positive breast cancer mouse cell line mimicking the immune microenvironment of anti-PD-1 resistant mammary carcinoma [ J Immunother Cancer, 2023, 11(6)e007117] | PubMed: 37344100 |
Sequential activation of E2F via Rb degradation and c-Myc drives resistance to CDK4/6 inhibitors in breast cancer [ Cell Rep, 2023, 42(11):113198] | PubMed: 37865915 |
Internally Controlled and Dynamic Optical Measures of Functional Tumor Biology [ Anal Chem, 2023, 95(13):5661-5670] | PubMed: 36952386 |
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。