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6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 combination of a different mTOR inhibitor temsirolimus (4 μM) and a different CDK4/6 inhibitor ribociclib (4 μM) is also synergistic against GICs (***P < 0.0001; one-way ANOVA with post-hoc Tukey analysis).

    Clin Cancer Res, 2017, 23(22):6958-6968. 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.

    SJSA cells were treated with the alternate CDK4/6 inhibitors Ribociclib (LEE011) and Abemaciclib (LY2835219) for 30 h, alone or in combination with Nutlin at 20 µM for 6 h.

    Cell Death Dis, 2018, 9(9): 918. 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 NYPWXVU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHqT4EzPCCq MVPHTVUxRTJ5NjDuUS=> MU[yOVg2OjB3OB?=
Myoblast NYTncWV{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjNRVQ4OiCq NF71NIdKSzVyPUGwN|Uhdk1? Mm\LNlU5OTB|N{W=
IMRS MnTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVGzUmEyPzJiaB?= MoDPTWM2OD16N{Ogcm0> NGm3W3MzPThzMEO3OS=>
SKNAS MoTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnSNHBSPzJiaB?= M4L2VWlEPTExvK6xNFAxOCCwTR?= Ml3BNlU5OTB|N{W=
Rh28 NWDVbnJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTVV2w4OiCq MkXGTWM2OD16NEWgcm0> M2LtZVI2QDFyM{e1
Rh41 M{\0Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYO3NkBp NYq2OXFvUUN3ME23NVg4KG6P Mkn4NlU5OTB|N{W=
CW9019 NFHZTlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWG3NkBp NUKyenZWUUN3ME25PVEzKG6P NIfqWYQzPThzMEO3OS=>
Rh5 MoP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWW3NkBp NETrc2tKSzVy78{eNVAxODBibl2= MUiyOVgyODN5NR?=
Rh30 MmrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\McW1jPzJiaB?= NVWwXHpOUUN3MP-8olExODByIH7N MYWyOVgyODN5NR?=
778 NVPE[YZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHEO|IhcA>? M3jK[YlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NETNRVUzPTB{OES2PS=>
449 M1LwUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvGfW1IPzJiaB?= M4XFdIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NGLCW|MzPTB{OES2PS=>
LP3 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPFOYI4OiCq MUDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M4DGWFI2ODJ6NE[5
LP6 NWK5ZmJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\MT3I4OiCq MnLvbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MUKyOVAzQDR4OR?=
LP8 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmG4O|IhcA>? Mn7ubY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NIW5PIkzPTB{OES2PS=>
LPS141 M37EZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzsUnY4OiCq NEToXmtqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NH\mUVYzPTB{OES2PS=>
778 NIm4[IFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{n6[VMvOzNizszN NFr2UnkzPCCq NE\GPYFl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> NV76NGlEOjVyMki0Olk>
449 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrQN{4{OyEQvF2= M1LVTFI1KGh? MVPk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= M1q3R|I2ODJ6NE[5
LP3 M4r3UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrvTFg5Oy5|MzFOwG0> MXGyOEBp MlP3[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= M4LvblI2ODJ6NE[5
LP6 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HyPFMvOzNizszN NGfGeIYzPCCq NGDLRXNl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> MlTYNlUxOjh2Nkm=
LP8 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfDfJczOy5|MzFOwG0> NYPuemV1OjRiaB?= NHru[IZl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> NUDSWo1ZOjVyMki0Olk>
LPS141 MonyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVizMlM{KM7:TR?= NHmzbJczPCCq NW\QNYRy\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> NXzpOFBCOjVyMki0Olk>
IMR5 MkjJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkT5NlQhcA>? MlTFSG1UVw>? MVPJR|UxRTF{NjDuUS=> MlqwNlQxPDVzN{m=
BE2C M2HXN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfGV5FzOjRiaB?= M3zvXWROW09? NYO1PJE4UUN3ME2xN|Qhdk1? NU\vXXhSOjRyNEWxO|k>
1643 M{LvZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvINlQhcA>? NEPUb5RFVVOR NWXpe3FiUUN3ME2xOFchdk1? MYiyOFA1PTF5OR?=
SKNSH NE\mcnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXq5PYpTOjRiaB?= M3;q[2ROW09? MUHJR|UxRTF2ODDuUS=> M1zrUFI1ODR3MUe5
SY5Y M1LDcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mle2NlQhcA>? NGS5flNFVVOR NV;4PJo6UUN3ME2xOVQhdk1? Mkf1NlQxPDVzN{m=
NGP NWj5Z|RsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzCNlQhcA>? NV7FUY9iTE2VTx?= MmexTWM2OD1zN{Wgcm0> MVeyOFA1PTF5OR?=
KELLY MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{S0dFI1KGh? NFvmPYJFVVOR MX\JR|UxRTJ{MDDuUS=> NVXJWGZwOjRyNEWxO|k>
CHP134 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7yNlQhcA>? NHG5XXRFVVOR MkTJTWM2OD1{N{Ogcm0> NFni[GwzPDB2NUG3PS=>
NLF NXvLTpVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;ENlQhcA>? MW\EUXNQ MVLJR|UxRTN{ODDuUS=> NGD3ZZEzPDB2NUG3PS=>
LAN5 M2H0cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLWd3dROjRiaB?= NUHmUJBHTE2VTx?= M1TMPWlEPTB;NEK5JI5O MXqyOFA1PTF5OR?=
NB69 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX2yOEBp NYfNdY5DTE2VTx?= MVrJR|UxRTd|ODDuUS=> M{n1WlI1ODR3MUe5
SKNDZ NYDaPWFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2WyNlI1KGh? M2[3RWROW09? NWrFdVZ3UUN3ME24NFEhdk1? NF76[GczPDB2NUG3PS=>
NBSD MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHrNlQhcA>? M4HJZmROW09? NHrtdYJKSzVyPUG5NFAhdk1? NXXpWo85OjRyNEWxO|k>
SKNF1 NV7Z[pk2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37YPFI1KGh? NXfi[29KTE2VTx?= NVnpSJRIUUN3ME2zOVAxKG6P MX2yOFA1PTF5OR?=
EBC1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnSxNlQhcA>? NILieGpFVVOR M{LSfWlEPTB;NkSwNEBvVQ>? M{PibFI1ODR3MUe5
SKNAS M2GzOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHHNlQhcA>? MoDxSG1UVw>? MVrJR|Ux97zgMUCwNFAhdk1? Ml;6NlQxPDVzN{m=
NB16 M4Tac2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmH1NlQhcA>? NYDNNmVCTE2VTx?= M1z0e2lEPTExvK6xNFAxOCCwTR?= NIfzbW8zPDB2NUG3PS=>
RPE1 M33tPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LHblI1KGh? MmnvSG1UVw>? MXLJR|Ux97zgMUCwNFAhdk1? MkDRNlQxPDVzN{m=

... 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
NCT03701334 Not yet recruiting Early Breast Cancer Novartis Pharmaceuticals|Translational Research in Oncology|Novartis December 27 2018 Phase 3
NCT03740334 Not yet recruiting Acute Lymphoblastic Leukemia ALL Dana-Farber Cancer Institute|Novartis November 30 2018 Phase 1
NCT03673124 Not yet recruiting Low Grade Serous Carcinoma Gynecologic Oncology Group|Novartis November 30 2018 Phase 2
NCT03613220 Not yet recruiting HR+ HER2 Breast Cancer Novartis Pharmaceuticals|Novartis October 30 2018 Phase 2
NCT03671330 Recruiting Breast Cancer Novartis Pharmaceuticals|Novartis August 29 2018 Phase 2
NCT03477396 Active not recruiting Estrogen Receptor and/or Progesterone Receptor Positive|HER2/Neu Negative|Stage IV Breast Cancer AJCC v6 and v7 City of Hope Medical Center|National Cancer Institute (NCI) June 14 2018 Phase 2

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操作手册

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CDK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID