Ribociclib (LEE011)

製品コード:S7440

For research use only.

Ribociclib (LEE011) is an orally available, and highly specific inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM. Phase 3.

Ribociclib (LEE011)化学構造

CAS No. 1211441-98-3

サイズ 価格(税別)
10mM (1mL in DMSO) JPY 44700
JPY 34700
JPY 51300
JPY 86960

代表番号: 03-5615-9297|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(64)

製品安全説明書

CDK阻害剤の選択性比較

相関CDK製品

生物活性

製品説明 Ribociclib (LEE011) is an orally available, and highly specific inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM. 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 [2]
(Cell-free assay)
CDK6 [2]
(Cell-free assay)
10 nM 39 nM
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 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LVV|I1KGh? MlLJS2k2OD1{N{[gcm0> NHnUXZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi1NlA2QCd-MkW4OVIxPTh:L3G+
Myoblast M2\peGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHtRoQ2PzJiaB?= Mo\JTWM2OD1zMEO1JI5O NYjHS|dERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NVA{PzVpPkK1PFExOzd3PD;hQi=>
IMRS MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlL3O|IhcA>? MXPJR|UxRTh5MzDuUS=> MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPThzMEO3OUc,OjV6MUCzO|U9N2F-
SKNAS MlXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnQTpA4OiCq NIPJNYFKSzVy78{eNVAxODBibl2= NEfBVXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUixNFM4PSd-MkW4NVA{PzV:L3G+
Rh28 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXO3NkBp M3zaTWlEPTB;OES1JI5O NXf3WGtpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NVA{PzVpPkK1PFExOzd3PD;hQi=>
Rh41 NYD6NXpMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkGxO|IhcA>? MYjJR|UxRTdzOEegcm0> NYDjcVNIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NVA{PzVpPkK1PFExOzd3PD;hQi=>
CW9019 NXTU[Zc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HMZVczKGh? NY\M[Iw{UUN3ME25PVEzKG6P NV3ISVNyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NVA{PzVpPkK1PFExOzd3PD;hQi=>
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Rh30 NUD2fVFRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXu3NkBp MUjJR|Ux97zgMUCwNFAhdk1? MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPThzMEO3OUc,OjV6MUCzO|U9N2F-
778 NWjsbpJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;xXlczKGh? NVfhe2hIcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NXPBeIw5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNlg1PjlpPkK1NFI5PDZ7PD;hQi=>
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LP8 NFq1NopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\yUFY4OiCq MVzpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB{OES2PUc,OjVyMki0Olk9N2F-
LPS141 NE\YU3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTmbFVRPzJiaB?= NES4V5pqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 Mn\mQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMki0OlkoRjJ3MEK4OFY6RC:jPh?=
778 Mmr3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XicVMvOzNizszN NIPCW2EzPCCq NGThPIll\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> NF;ENoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCyPFQ3QSd-MkWwNlg1Pjl:L3G+
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LP3 M{i4[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjvN{4{OyEQvF2= M{HhR|I1KGh? NFj3Xnhl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB{OES2PUc,OjVyMki0Olk9N2F-
LP6 NHvHbZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLz[HpUOy5|MzFOwG0> NG[wVoMzPCCq M4qx[IRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl M17ISlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEK4OFY6Lz5{NUCyPFQ3QTxxYU6=
LP8 M{e1[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFKxT3g{NjN|IN88US=> MnSxNlQhcA>? NX3wXmlC\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> M1zZeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEK4OFY6Lz5{NUCyPFQ3QTxxYU6=
LPS141 NGKybG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYWzMlM{KM7:TR?= MkHENlQhcA>? MV;k[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NYXRT5lSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNlg1PjlpPkK1NFI5PDZ7PD;hQi=>
IMR5 NEXtWpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFe4eIwzPCCq M4LOdGROW09? MVvJR|UxRTF{NjDuUS=> NWLiW25[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOFUyPzlpPkK0NFQ2OTd7PD;hQi=>
BE2C M4OxcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTHfZQzPCCq M3HQc2ROW09? NIrLNlNKSzVyPUGzOEBvVQ>? NGK2dGo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC0OVE4QSd-MkSwOFUyPzl:L3G+
1643 MnvWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVeyOEBp NWHZSZk5TE2VTx?= NEXFSolKSzVyPUG0O{BvVQ>? NVi3WIFSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOFUyPzlpPkK0NFQ2OTd7PD;hQi=>
SKNSH NHvTT4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLLNlQhcA>? NXfP[|JrTE2VTx?= MnXWTWM2OD1zNEigcm0> NIn5c5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC0OVE4QSd-MkSwOFUyPzl:L3G+
SY5Y M4PtfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHDNlQhcA>? Mnv1SG1UVw>? Mo\tTWM2OD1zNUSgcm0> NH7ZemQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC0OVE4QSd-MkSwOFUyPzl:L3G+
NGP M3;NR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\zboMzPCCq M3qwWWROW09? NVXRTox7UUN3ME2xO|Uhdk1? MoPlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNEWxO|koRjJ2MES1NVc6RC:jPh?=
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CHP134 NEXaeW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXm0dol1OjRiaB?= NUfnZYV{TE2VTx?= M2f3TWlEPTB;MkezJI5O M{PhVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MES1NVc6Lz5{NEC0OVE4QTxxYU6=
NLF MlXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYqyOEBp MmXsSG1UVw>? MUfJR|UxRTN{ODDuUS=> NVjxdJh[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOFUyPzlpPkK0NFQ2OTd7PD;hQi=>
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KOPN8 NX;SOlhGSXCxcITvd4l{KGG|c3H5 MVWwMlUhfU1? M2jIZ|I1KGi{cx?= MX;JcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEuRUF64JINmdGy|IHHzd4V{e2WmIHHzJJVxemWpdXzheIlwdiCxZjDjcIVifmWmIGDBVnAhdGW4ZXygZZQhOC53IIXNJJBz\S22cnXheIVlKHerdHigUmFEKG[xcjCxJIhzKGGwZDDt[YF{fXKnZDDh[pRmeiB{NDDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTRyN{m3OUc,Ojl2MEe5O|U9N2F-
Hep3B NX63boExS2WubDDjfYNt\SCjc4PhfS=> NXvEZYVXOjRiaILz MY\D[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDI[ZA{SiClZXzsd{Bie3Onc4Pl[EBieyCjY3P1cZVt[XSrb36gZZQhTzBxR{GgdIhie2ViYX\0[ZIhOjRiaILzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcoch[mG|ZXSg[oxwfyCleYTvcYV1enl? NXryc5RHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NVg{OTJpPkK5OVE5OzF{PD;hQi=>
HepG2 NIDQbGRE\WyuIHP5Z4xmKGG|c3H5 Mm\3NlQhcHK| NXyzNGxUS2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IFewM2cyKHCqYYPlJIFnfGW{IEK0JIhzeyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pIHLhd4VlKG[ub4egZ5l1d22ndIL5 MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTVzOEOxNkc,Ojl3MUizNVI9N2F-
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アッセイ
Methods Test Index PMID
Western blot pRb(S807) / Rb / p53 / Cyclin E / Cyclin D1 / CDK4 / CDK6 / p27 / p21 / PARP 29789630
Growth inhibition assay Cell viability 26390342
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]

  • 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.

動物試験:

[1]

  • 動物モデル:Mice bearing BE2C, NB-1643, or EBC1 xenografts.
  • 投薬量:~200 mg/kg daily
  • 投与方法:p.o.

溶解度 (25°C)

体外

化学情報

分子量 434.54
化学式

C23H30N8O

CAS No. 1211441-98-3
Storage 3年 -20°C
2年 -80°C in solvent
Smiles CN(C)C(=O)C1=CC2=CN=C(N=C2N1C3CCCC3)NC4=NC=C(C=C4)N5CCNCC5

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

便利ツール

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05429502 Not yet recruiting Drug: Topotecan|Drug: Temozolomide|Drug: Ribociclib Neuroblastoma Novartis Pharmaceuticals|Innovative Therapies For Children with Cancer Consortium|Novartis August 31 2022 Phase 1|Phase 2
NCT04657679 Recruiting Drug: Ribociclib Breast Cancer Georgetown University|Medstar Health Research Institute|Breast Cancer Research Foundation|Georgetown-Howard Universities Center for Clinical and Translational Science (GHUCCTS) May 20 2021 Phase 4
NCT04315233 Recruiting Drug: Ribociclib|Drug: Belinostat Metastatic Breast Cancer|Recurrent Ovarian Carcinoma University of Utah|Novartis|Acrotech Biopharma May 3 2021 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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。

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Tags: Ribociclib (LEE011)を買う | Ribociclib (LEE011) ic50 | Ribociclib (LEE011)供給者 | Ribociclib (LEE011)を購入する | Ribociclib (LEE011)費用 | Ribociclib (LEE011)生産者 | オーダーRibociclib (LEE011) | Ribociclib (LEE011)化学構造 | Ribociclib (LEE011)分子量 | Ribociclib (LEE011)代理店