Ribociclib (LEE011)

製品コードS7440

Ribociclib (LEE011)化学構造

分子量(MW):434.54

Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor. Phase 3.

サイズ 価格(税別)  
JPY 32702.00
JPY 49302.00

カスタマーフィードバック(6)

  • 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.

製品安全説明書

CDK阻害剤の選択性比較

生物活性

製品説明 Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor. Phase 3.
特性 Orally bioavailable CDK4/6-selective inhibitor that has been tested in Phase III clinical trials for treatment of advanced breast cancer.
ターゲット
CDK4 [1]
(Cell-free assay)
CDK6 [1]
(Cell-free assay)
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
DFSP105 NEjBSWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYKyOEBp MmjjS2k2OD1{N{[gcm0> M2rhRVI2QDV{MEW4
Myoblast NWHTcFdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rEZlczKGh? MUTJR|UxRTFyM{Wgcm0> M4r3NlI2QDFyM{e1
IMRS NUHEU4xLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zkcFczKGh? NXnufnlLUUN3ME24O|Mhdk1? NYXNWFY4OjV6MUCzO|U>
SKNAS NVz1d4w4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnmdowzPzJiaB?= MlfITWM2OO,:nkGwNFAxKG6P MV2yOVgyODN5NR?=
Rh28 M2KzZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\BO|IhcA>? NWLNTpVDUUN3ME24OFUhdk1? NWTINYNvOjV6MUCzO|U>
Rh41 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{W5[|czKGh? NUG5RYVrUUN3ME23NVg4KG6P M1HuNlI2QDFyM{e1
CW9019 M1fjdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXwO|IhcA>? NEjMeodKSzVyPUm5NVIhdk1? NVizZmE6OjV6MUCzO|U>
Rh5 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml21O|IhcA>? NF3ZdY1KSzVy78{eNVAxODBibl2= MXeyOVgyODN5NR?=
Rh30 NUfndlhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW[3NkBp MmPpTWM2OO,:nkGwNFAxKG6P MXqyOVgyODN5NR?=
778 NXH3UGt4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUe3NkBp NUjDNWt6cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NUDm[lhCOjVyMki0Olk>
449 NWi4T4tMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIflTWM4OiCq NWLMVFV5cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NHT5bXAzPTB{OES2PS=>
LP3 NEnndotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkGxO|IhcA>? MoHvbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NFfQOZAzPTB{OES2PS=>
LP6 NV;KTpRST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHZZow4OiCq MXzpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NGXoUYczPTB{OES2PS=>
LP8 NGrMSZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUW3NkBp MXvpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MUiyOVAzQDR4OR?=
LPS141 NFHseVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXOO|IhcA>? Mn3hbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MV[yOVAzQDR4OR?=
778 MoDiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXf6ephGOy5|MzFOwG0> M4\CUVI1KGh? MWTk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NYS4eVBSOjVyMki0Olk>
449 NWC0bnA5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjnN{4{OyEQvF2= M4DHWFI1KGh? NFLremtl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> M3O3dFI2ODJ6NE[5
LP3 MoTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXGzMlM{KM7:TR?= NVP4bI5pOjRiaB?= MXLk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= M2LVUVI2ODJ6NE[5
LP6 M4fUZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;KN{4{OyEQvF2= NIPHRWkzPCCq NYK4c3F7\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> NGrMbowzPTB{OES2PS=>
LP8 MkGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\SN{4{OyEQvF2= NWXrOYhsOjRiaB?= NV\qc4FE\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> NEm0Z48zPTB{OES2PS=>
LPS141 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvL[5c2Oy5|MzFOwG0> MYKyOEBp NXLwZWZ6\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> M3jrfVI2ODJ6NE[5
IMR5 MmDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWKyOEBp M13VcmROW09? MW\JR|UxRTF{NjDuUS=> NH\WTHgzPDB2NUG3PS=>
BE2C MmHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3QNlQhcA>? M1X3[GROW09? MmHGTWM2OD1zM{Sgcm0> Mk[yNlQxPDVzN{m=
1643 MnmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{j5[|I1KGh? MkXHSG1UVw>? MWPJR|UxRTF2NzDuUS=> MmfRNlQxPDVzN{m=
SKNSH NX;Uc3ZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYiyOEBp NFSyRWpFVVOR MYTJR|UxRTF2ODDuUS=> MljFNlQxPDVzN{m=
SY5Y NEjuVlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{L2OFI1KGh? MlPHSG1UVw>? Ml;xTWM2OD1zNUSgcm0> M{e1ZlI1ODR3MUe5
NGP M3;0emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUH4VJNUOjRiaB?= MmDwSG1UVw>? M1flc2lEPTB;MUe1JI5O Mo\ONlQxPDVzN{m=
KELLY NI\nfXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjkVXlOOjRiaB?= NXTqdJI{TE2VTx?= M1mwWWlEPTB;MkKwJI5O MWeyOFA1PTF5OR?=
CHP134 NYP5V5RCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHm[|IzPCCq NGnjSYJFVVOR NUPBVGJpUUN3ME2yO|Mhdk1? MmfGNlQxPDVzN{m=
NLF NH7mO5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnG[m9NOjRiaB?= MWHEUXNQ NHXwcG1KSzVyPUOyPEBvVQ>? M{Tld|I1ODR3MUe5
LAN5 MkTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmG5NlQhcA>? NXW4bJd[TE2VTx?= NX;HVHVQUUN3ME20Nlkhdk1? M37jZVI1ODR3MUe5
NB69 MlTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY[yOEBp MkSxSG1UVw>? MlnHTWM2OD15M{igcm0> M{nZOVI1ODR3MUe5
SKNDZ MlzTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPLU4lvOjRiaB?= NFm0TG9FVVOR M1XBOGlEPTB;OECxJI5O NV2xPFc2OjRyNEWxO|k>
NBSD M4rsSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVSyOEBp NHfFbWdFVVOR MULJR|UxRTF7MECgcm0> MlflNlQxPDVzN{m=
SKNF1 MlfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXSyOEBp MnLLSG1UVw>? NEPiPG1KSzVyPUO1NFAhdk1? MVqyOFA1PTF5OR?=
EBC1 NGrGSHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\Fe4EzPCCq MVnEUXNQ MXzJR|UxRTZ2MECgcm0> NWe4XYljOjRyNEWxO|k>
SKNAS MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkK0NlQhcA>? MlHuSG1UVw>? M1XBN2lEPTExvK6xNFAxOCCwTR?= NFvhZ4wzPDB2NUG3PS=>
NB16 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXsUpNCOjRiaB?= NXrub2VrTE2VTx?= NGPhU2xKSzVy78{eNVAxODBibl2= NGLzeo0zPDB2NUG3PS=>
RPE1 MmjQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4G0eFI1KGh? MmW1SG1UVw>? MWHJR|Ux97zgMUCwNFAhdk1? NYrpZ3Z3OjRyNEWxO|k>

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 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]

お薦めの試験操作(参考用のみ)

細胞試験:

[1]

+ 展開
  • 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.


    (参考用のみ)
動物試験:

[1]

+ 展開
  • 動物モデル: Mice bearing BE2C, NB-1643, or EBC1 xenografts.
  • 製剤: 0.5% methylcellulose
  • 投薬量: ~200 mg/kg daily
  • 投与方法: p.o.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 7 mg/mL (16.1 mM)
Water Insoluble
Ethanol Insoluble

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 434.54
化学式

C23H30N8O

CAS No. 1211441-98-3
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03822468 Not yet recruiting Breast Cancer Novartis Pharmaceuticals|Novartis October 30 2019 Phase 2
NCT03822468 Not yet recruiting Breast Cancer Novartis Pharmaceuticals|Novartis October 30 2019 Phase 2
NCT03613220 Not yet recruiting HR+ HER2 Breast Cancer Novartis Pharmaceuticals|Novartis April 1 2019 Phase 2
NCT03613220 Not yet recruiting HR+ HER2 Breast Cancer Novartis Pharmaceuticals|Novartis April 1 2019 Phase 2
NCT03839823 Not yet recruiting Breast Cancer Novartis Pharmaceuticals|Novartis February 28 2019 Phase 2
NCT03839823 Not yet recruiting Breast Cancer Novartis Pharmaceuticals|Novartis February 28 2019 Phase 2

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

CDKシグナル伝達経路

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID