Ribociclib (LEE011)
目录号：S7440
Molecular Weight(MW): 434.54
Ribociclib (LEE011)是一种口服具有活性的，高度特异性CDK4/6抑制剂。Phase 3。
客户使用该产品的4个实验数据：
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IB analysis of whole cell lysates derived from mouse CT26 or 4T1 tumor cell lines treated with or without the CDK4/6 inhibitor, ribociclib.
Nature, 2017, 553(7686):91-95. Ribociclib (LEE011) purchased from Selleck.
The effects of the CDK inhibitor abemaciclib, palbociclib, and ribociclib on Trop2 ICD cleavage. CDK inhibitors decreased Trop2 ICD abundance after the second day of CDK inhibitor treatment.
Cancer Res, 2016, 76(22):6723-6734. Ribociclib (LEE011) purchased from Selleck.
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(B) The effects of AZD2014, BEZ235, lapatinib, LEE011, pazopanib on PI3K/AKT signaling in sarcoma PDC line were determined by immunoblotting analysis. Cells were treated with 1 μM of the indicated drugs for 72 h.
Transl Oncol, 2016, 9(3):197-202.. Ribociclib (LEE011) purchased from Selleck.
Analysis of apoptosis in leukemia cells induced by LEE011. Annexin V staining of cells following 48-h treatment with LEE011 at 2 or 5 µM compared with DMSO controls. Following 5-µM LEE011 treatment, the K562 apoptotic cell percentage was 5.9 ± 0.75 vs. 1.2 ± 0.66% for the DMSO group, P = 0.001; in MV4-11 cells, the apoptotic cell percentage was 24.2 ± 3.06 vs. 0.53 ± 0.40% for the DMSO group, P = 0.005; in U937 cells, the apoptotic cell percentage was 9.9 ± 2.81 vs. 0.57 ± 0.42% for the DMSO group, P = 0.027; in HL-60 cells, the apoptotic cell percentage was 28.23 ± 6.01 vs. 0.9 ± 0.8% for the DMSO group, P = 0.015; in THP-1 cells, the apoptotic cell percentage was 1.76 ± 0.4 vs. 1.56 ± 0.45% for the DMSO group, P = 0.59; in CCRF cells, the apoptotic cell percentage was 13.77 ± 3.16 vs. 1.2 ± 0.36% for the DMSO group, P = 0.019; in NB4 cells, the apoptotic cell percentage was 12.1 ± 1.35 vs. 0.86 ± 0.25% for the DMSO group, P = 0.004; and in SHI-1 cells the apoptotic cell percentage was 12.6 ± 2.81 vs. 1.87 ± 0.75% for the DMSO group, P = 0.017. These analyses were repeated three times. *P < 0.05; **P < 0.01
Cancer Cell Int, 2017, 17:35. Ribociclib (LEE011) purchased from Selleck.
产品安全说明书
CDK抑制剂选择性比较
生物活性
| 产品描述 | Ribociclib (LEE011)是一种口服具有活性的，高度特异性CDK4/6抑制剂。Phase 3。 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 特性 | 口服生物有效的CDK4/6选择性抑制剂，处于Ⅲ期临床测试，用于晚期乳腺癌的治疗。 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 靶点 |
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| 体外研究 |
LEE011是一种CDK4/CDK6的双重抑制剂，能够显著抑制17种神经细胞瘤中的12种的生长，平均IC50值是307 nM。对神经细胞瘤的抑制主要是抑制细胞的生长，受到G1细胞周期阻滞和细胞衰老的调控。 |
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| Cell Data |
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| 体内研究 | LEE011 (200 mg/kg 每日，口服)引起小鼠中的BE2C 或者 1643细胞显著的生长延迟，没有体重减轻或者其它的毒性症状。[1] |
推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)
| 细胞实验： |
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| 动物实验： |
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溶解度 (25°C)
| 体外 | DMSO | 7 mg/mL (16.1 mM) |
|---|---|---|
| Water | Insoluble | |
| Ethanol | Insoluble |
* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。
化学数据
| 分子量 | 434.54 |
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| 化学式 | C23H30N8O |
| CAS号 | 1211441-98-3 |
| 稳定性 | powder |
| in solvent | |
| 别名 | N/A |
计算器
摩尔浓度计算器
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。
稀释计算器
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )
在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.
分子量计算器
通过输入化合物的化学式来计算其分子量：
注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2
摩尔浓度计算器
临床试验信息
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02657343 | Recruiting | Breast Cancer | Dana-Farber Cancer Institute|Novartis | March 9 2016 | Phase 1|Phase 2 |
| NCT02422615 | Active not recruiting | Breast Neoplasms|Breast Diseases|Neoplasms|Neoplasms by Site|Fulvestrant|Antineoplastic Agents|Antineoplastic Agents Hormonal|Estrogen Receptor Antagonists|Hormone Antagonists|Hormones Hormone Substitutes and Hormone Antagonists|Molecular Mechanisms of Pharmacological Action|Pharmacologic Actions|Therapeutic Use | Novartis Pharmaceuticals|Novartis | June 9 2015 | Phase 3 |
| NCT03114527 | Recruiting | Soft Tissue Sarcoma | Fox Chase Cancer Center | August 8 2017 | Phase 2 |
| NCT02657928 | Active not recruiting | Estrogen Receptor Positive|Postmenopausal|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Recurrent Uterine Corpus Carcinoma | Mayo Clinic|National Cancer Institute (NCI) | July 8 2016 | Phase 2 |
| NCT01857193 | Active not recruiting | Breast Cancer | Novartis Pharmaceuticals|Novartis | September 6 2013 | Phase 1 |
| NCT03434262 | Recruiting | Anaplastic Astrocytoma|Anaplastic Ependymoma|Anaplastic Ganglioglioma|Anaplastic Meningioma|Anaplastic Oligodendroglioma|Pleomorphic Xanthoastrocytoma Anaplastic|Atypical Teratoid/Rhabdoid Tumor|Brain Cancer|Brain Tumor|Central Nervous System Neoplasms|Choroid Plexus Carcinoma|CNS Embryonal Tumor With Rhabdoid Features|Ganglioneuroblastoma of Central Nervous System|CNS Tumor|Embryonal Tumor of CNS|Ependymoma|Glioblastoma|Glioma|Glioma Malignant|Medulloblastoma|Medulloblastoma; Unspecified Site|Medulloepithelioma|Neuroepithelial Tumor|Neoplasms|Neoplasms Neuroepithelial|Papillary Tumor of the Pineal Region (High-grade Only)|Pediatric Brain Tumor|Pineal Parenchymal Tumor of Intermediate Differentiation (High-grade Only)|Pineoblastoma|Primitive Neuroectodermal Tumor|Recurrent Medulloblastoma|Refractory Brain Tumor|Neuroblastoma. CNS|Glioblastoma IDH-mutant|Glioblastoma IDH-wildtype|Medulloblastoma Group 3|Medulloblastoma Group 4|Glioma High Grade|Neuroepithelial Tumor High Grade|Medulloblastoma SHH-activated and TP53 Mutant|Medulloblastoma SHH-activated and TP53 Wildtype|Medulloblastoma Chromosome 9q Loss|Medulloblastoma Non-WNT Non-SHH NOS|Medulloblastoma Non-WNT/Non-SHH|Medulloblastoma PTCH1 Mutation|Medulloblastoma WNT-activated|Ependymoma Recurrent|Glioma Recurrent High Grade|Glioma Recurrent Malignant|Embryonal Tumor NOS|Glioma Diffuse Midline H3K27M-mutant|Embryonal Tumor With Multilayered Rosettes (ETMR)|Ependymoma NOS WHO Grade III|Ependymoma NOS WHO Grade II|Medulloblastoma G3/G4|Ependymoma RELA Fusion Positive | St. Jude Children''s Research Hospital|Novartis Pharmaceuticals | March 5 2018 | Phase 1 |
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