瑞博西尼|T6199

Ribociclib
1211441-98-3

￥233 1mg 起订

￥329 2mg 起订

￥535 5mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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产品详情:

中文名称：: 瑞博西尼

英文名称：: Ribociclib

CAS号：: 1211441-98-3

品牌：: TargetMol

产地：: 美国

保存条件：: store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.96%

产品类别：: 抑制剂

货号：: T6199

Product Introduction

Bioactivity

名称	Ribociclib
描述	Ribociclib (LEE011) is a cell cycle protein-dependent kinase CDK4/6 inhibitor (IC50 = 10/39 nM) with specific and oral activity. Ribociclib has antitumor activity that blocks the cell cycle and inhibits tumor cell proliferation.
细胞实验	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. (Only for Reference)
激酶实验	Enzyme assays are performed using a homogeneous time-resolved fluorescence assay with recombinant epitope tagged kinase domains (JAK1, 837-1142; JAK2, 828-1132; JAK3, 718-1124; Tyk2, 873-1187) or full-length enzyme (cMET and Chk2) and peptide substrate. Each enzyme reaction is performed with or without test compound (11-point dilution), JAK, cMET, or Chk2 enzyme, 500 nM (100 nM for Chk2) peptide, ATP (at the Km specific for each kinase or 1 mM), and 2.0% DMSO in assay buffer. The calculated IC50 value is the compound concentration required for inhibition of 50% of the fluorescent signal. Additional kinase assays are performed at Cerep using standard conditions at 200 nM. Enzymes tested included: Abl, Akt1, AurA, AurB, CDC2, CDK2, CDK4, CHK2, c-kit, EGFR, EphB4, ERK1, ERK2, FLT-1, HER2, IGF1R, IKKα, IKKβ, JNK1, Lck, MEK1, p38α, p70S6K, PKA, PKCα, Src, and ZAP70[1].
体外活性	方法：人乳腺癌细胞 MDA-MB-231 用 Ribociclib (0-20 µM) 处理 24-144 h，使用 CCK8 assay 检测细胞活力。结果：Ribociclib 抑制 MDA-MB-231 中的细胞增殖。[1] 方法：神经母细胞瘤细胞系 BE2C、IMR5、EBC1 和 SKNAS 用 Ribociclib (0.01-10 µM) 处理 96 h，使用 Western Blot 检测靶点蛋白表达水平。结果：在 BE2C 和 IMR5 细胞系中，从 250 nM 开始观察到 pRBS780 的耗竭。在 EBC1 和 SKNAS 抗性细胞系中也观察到 pRBS780 的降低，但仅在较高的抑制剂浓度下。[2]
体内活性	方法：为测试体内抗肿瘤活性，将 Ribociclib (200 mg/kg in 0.5 % methylcellulose) 口服给药给携带神经母细胞瘤 BE2C、NB-1643 或 EBC1 的 CB17 小鼠，每天一次，持续二十一天。结果：在携带 BE2C 或 1643 异种移植物的小鼠中，肿瘤生长在整个 21 天的治疗过程中显著延迟。在 EBC1 异种移植物模型中，肿瘤生长抑制不那么有力。[2]
存储条件	store under nitrogen \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 50 mg/mL (115.06 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (11.51 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. Ethanol : < 1 mg/mL (insoluble or slightly soluble)
关键字	Cyclin dependent kinase \| inhibit \| Inhibitor \| LEE 011 \| Ribociclib \| CDK \| LEE-011
相关产品	Sodium Oxamate \| Axitinib \| CASIN \| Sorafenib tosylate \| Lenvatinib mesylate \| Regorafenib \| Pazopanib \| Nintedanib \| Sorafenib \| Regorafenib monohydrate \| Dinaciclib \| Abemaciclib
相关库	经典已知活性库 \| 抗癌活性化合物库 \| 激酶抑制剂库 \| EMA 上市药物库 \| 酪氨酸激酶分子库 \| 抗癌临床化合物库 \| 抗癌药物库

瑞博西尼|||LEE011|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子