Ribociclib

製品コードS7440 バッチS744002

印刷

化学情報

Chemical Structure Synonyms LEE011 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C23H30N8O
分子量 434.54 CAS No. 1211441-98-3
Solubility (25°C)* 体外 DMSO 7 mg/mL (16.1 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.

溶剤液（一定の濃度）を調合する

生物活性

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.
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.

プロトコル(参考用のみ)

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.
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.
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.

カスタマーフィードバック

, , 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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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。

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