Ribociclib (LEE011)

目录号:S7440

Ribociclib (LEE011) Chemical Structure

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。

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RMB 2447.92 现货
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客户使用该产品的4个实验数据:

  • 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.

  • (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。
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
CDK4 [1]
(Cell-free assay)
CDK6 [1]
(Cell-free assay)
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。

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
DFSP105 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUmyOEBp NYLTe2dKT0l3ME2yO|Yhdk1? NVrSSJlpOjV6NUKwOVg>
Myoblast NUn4XJNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\pRlczKGh? M4TKT2lEPTB;MUCzOUBvVQ>? M3zRcVI2QDFyM{e1
IMRS Mon6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;BdYRCPzJiaB?= NF75ZoxKSzVyPUi3N{BvVQ>? M{T1OlI2QDFyM{e1
SKNAS NX;jbWJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfvfm9lPzJiaB?= MmrrTWM2OO,:nkGwNFAxKG6P M{fCdVI2QDFyM{e1
Rh28 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HrNlczKGh? M1vEZWlEPTB;OES1JI5O M4HZbFI2QDFyM{e1
Rh41 NEL5XnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYO3NkBp M3;JW2lEPTB;N{G4O{BvVQ>? NVy0WI5NOjV6MUCzO|U>
CW9019 NEjTfpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrORYJpPzJiaB?= NIXhV2JKSzVyPUm5NVIhdk1? M{TVeVI2QDFyM{e1
Rh5 M{DPeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLn[mMyPzJiaB?= MnHKTWM2OO,:nkGwNFAxKG6P NGHvVI4zPThzMEO3OS=>
Rh30 M1nMXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPyO|IhcA>? M3fZN2lEPTExvK6xNFAxOCCwTR?= NWfnb2JPOjV6MUCzO|U>
778 MlTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVe0XXB2PzJiaB?= MXzpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M1XKd|I2ODJ6NE[5
449 NXPzRoY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYH0d2R5PzJiaB?= NFfvcHdqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NU\0cmdGOjVyMki0Olk>
LP3 MlXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELoOZA4OiCq M3HRZYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MVOyOVAzQDR4OR?=
LP6 MnzPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnXO2pUPzJiaB?= MYXpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NWjRNXRqOjVyMki0Olk>
LP8 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{W2[|czKGh? MVzpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MkK5NlUxOjh2Nkm=
LPS141 Ml;yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnoO|IhcA>? MWPpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NGq1ZmkzPTB{OES2PS=>
778 M{fRZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{GyXFMvOzNizszN MnPoNlQhcA>? MV;k[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NWjmN|M6OjVyMki0Olk>
449 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDq[VdbOy5|MzFOwG0> M1fXVlI1KGh? MWPk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NWrSd2pzOjVyMki0Olk>
LP3 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFe2WJY{NjN|IN88US=> NYDBS4hnOjRiaB?= M3nWSYRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl MUmyOVAzQDR4OR?=
LP6 MmDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLRemFVOy5|MzFOwG0> M4X2fVI1KGh? M17nc4Rm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl MlXaNlUxOjh2Nkm=
LP8 NGWySmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYX3PFZ7Oy5|MzFOwG0> NE[zfGIzPCCq M1zIN4Rm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl Ml\NNlUxOjh2Nkm=
LPS141 NIrpUWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUOzMlM{KM7:TR?= NVPFRZRMOjRiaB?= Mlq2[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= NUK5bmNuOjVyMki0Olk>
IMR5 NFPIPWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjFO2MzPCCq MUXEUXNQ MoKyTWM2OD1zMk[gcm0> M3q1[FI1ODR3MUe5
BE2C MmW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLXNlQhcA>? MmrNSG1UVw>? NGCzdFFKSzVyPUGzOEBvVQ>? MX[yOFA1PTF5OR?=
1643 NH7IT5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3[yZlI1KGh? NIfZ[ZdFVVOR MXPJR|UxRTF2NzDuUS=> NWnGO2ZrOjRyNEWxO|k>
SKNSH NFjzTWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrkOJNEOjRiaB?= NHX5XopFVVOR NYXaUIo2UUN3ME2xOFghdk1? NUD3NW8zOjRyNEWxO|k>
SY5Y Ml;2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjVNlQhcA>? M1y3NmROW09? MmHnTWM2OD1zNUSgcm0> NF\oNpgzPDB2NUG3PS=>
NGP MknDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\W[HMzPCCq M3jaN2ROW09? M{jBbWlEPTB;MUe1JI5O Mli0NlQxPDVzN{m=
KELLY Mli1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXqyOEBp NUflNIpLTE2VTx?= M1nPeWlEPTB;MkKwJI5O NVe1WoNnOjRyNEWxO|k>
CHP134 M3exOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfRbWQzPCCq MkjmSG1UVw>? NIfwbIxKSzVyPUK3N{BvVQ>? M13LOFI1ODR3MUe5
NLF NUDkd3RbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TGbFI1KGh? MV3EUXNQ MkTZTWM2OD1|Mkigcm0> NXnFcYxjOjRyNEWxO|k>
LAN5 NXLRSlNRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33RWlI1KGh? M4fO[WROW09? Mli2TWM2OD12Mkmgcm0> MYmyOFA1PTF5OR?=
NB69 NHruTFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fvelI1KGh? MXvEUXNQ MUnJR|UxRTd|ODDuUS=> MVWyOFA1PTF5OR?=
SKNDZ M3r6W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLmNlQhcA>? NW\FPVBQTE2VTx?= NEjLXmpKSzVyPUiwNUBvVQ>? Mm[5NlQxPDVzN{m=
NBSD NYj1W4xlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\pNlQhcA>? MWHEUXNQ NVnHS2RSUUN3ME2xPVAxKG6P NVjOT5BxOjRyNEWxO|k>
SKNF1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4my[|I1KGh? NILnbHJFVVOR MnXPTWM2OD1|NUCwJI5O NHPrcGozPDB2NUG3PS=>
EBC1 M2\xVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{C1V|I1KGh? NIPuWVlFVVOR NIfWXXVKSzVyPU[0NFAhdk1? M{OzdVI1ODR3MUe5
SKNAS NGXQV29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DnVFI1KGh? MYrEUXNQ MXrJR|Ux97zgMUCwNFAhdk1? NHTmSYYzPDB2NUG3PS=>
NB16 NELDc5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILyNmszPCCq MU\EUXNQ M1nDU2lEPTExvK6xNFAxOCCwTR?= MlLUNlQxPDVzN{m=
RPE1 NVHvR2dWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PX[FI1KGh? NVPNWoh5TE2VTx?= MmWwTWM2OO,:nkGwNFAxKG6P MYqyOFA1PTF5OR?=

... Click to View More Cell Line Experimental Data

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:

[1]

+ 展开
  • Cell lines: BE2C, IMR5, 1643, SY5Y, CHP134, SKNSH, NGP, KELLY, LAN5, NLF, NB69, SKNDZ, NBSD, NBLS, SKNFI, EBC1, SKNAS, NB16, RPE1细胞系。
  • Concentrations: 10 μM
  • Incubation Time: ~100小时
  • Method:

    将板中优先附着基底生长的神经母细胞瘤细胞系以一式三份种植于Xcelligence实时细胞电子传感系统,用4个剂量梯度的抑制剂和DMSO为对照处理细胞24小时。连续监测细胞约100个小时,IC50通过以下方法测得:通过绘制细胞指数为时间的函数产生生长曲线,以在治疗开始时细胞指数为1作为标准。从治疗开始到处理96小时后,生长曲线下的面积通过基线下面积为1(治疗开始时的细胞指数)进行计算。积分面积以DMSO处理的对照组作为背景。抑制剂比上对照组的值取非线性对数值来计算。所有的实验至少重复一次。


    (Only for Reference)
动物实验:

[1]

+ 展开
  • Animal Models: BE2C, NB-1643,或EBC1异种移植的小鼠。
  • Formulation: 0.5%甲基纤维素
  • Dosages: ~200毫克/千克 每天
  • Administration: 口服
    (Only for Reference)

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
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

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

  • 质量
    浓度
    体积
    分子量

*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

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 )

  • C1
    V1
    C2
    V2

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。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID