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(4)

  • 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.

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 NHW4e2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDyNlQhcA>? NEPCeJVIUTVyPUK3OkBvVQ>? MWmyOVg2OjB3OB?=
Myoblast MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYK3NkBp M4TJNGlEPTB;MUCzOUBvVQ>? NVPiVlBqOjV6MUCzO|U>
IMRS M1;N[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYi3NkBp NXHsO|lLUUN3ME24O|Mhdk1? NWTycplbOjV6MUCzO|U>
SKNAS NIDvWXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3Q[2dkPzJiaB?= MVjJR|Ux97zgMUCwNFAhdk1? M4LEWFI2QDFyM{e1
Rh28 MnXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPVO|IhcA>? NF\YNlRKSzVyPUi0OUBvVQ>? MU[yOVgyODN5NR?=
Rh41 MnrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVO3NkBp M17SVmlEPTB;N{G4O{BvVQ>? NYnqTG43OjV6MUCzO|U>
CW9019 M1rzOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTESI9kPzJiaB?= NFToNJdKSzVyPUm5NVIhdk1? M4LXNVI2QDFyM{e1
Rh5 MnLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnBXJJuPzJiaB?= Mn;vTWM2OO,:nkGwNFAxKG6P MoXsNlU5OTB|N{W=
Rh30 MmfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX[3NkBp NXiyXIhPUUN3MP-8olExODByIH7N M2fWclI2QDFyM{e1
778 MkXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnz5O|IhcA>? M4riO4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NHjiU2IzPTB{OES2PS=>
449 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\rUnA4OiCq NI\JSZlqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MWmyOVAzQDR4OR?=
LP3 NVr4Upo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPMO|IhcA>? MUDpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MmD2NlUxOjh2Nkm=
LP6 NXfCepRJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnywO|IhcA>? MWjpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MkjCNlUxOjh2Nkm=
LP8 NFSxcVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\MN2I4OiCq NWfDNoY1cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NXPGXnpsOjVyMki0Olk>
LPS141 NInxV2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfNNG5[PzJiaB?= Mn\RbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> Ml\JNlUxOjh2Nkm=
778 M{DtVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXZNYNjOy5|MzFOwG0> NH32Um8zPCCq MkD3[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= NIrneFUzPTB{OES2PS=>
449 MnnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEi2TpA{NjN|IN88US=> MmD0NlQhcA>? M4rnUIRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl M371PVI2ODJ6NE[5
LP3 NX\Hd5RXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLYOY4{NjN|IN88US=> MoXBNlQhcA>? M1XWXIRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl NV\UTG16OjVyMki0Olk>
LP6 NHrZcGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnLNFA{NjN|IN88US=> M3WxXlI1KGh? NWfhVIFu\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> NFzxeWkzPTB{OES2PS=>
LP8 M17k[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XD[FMvOzNizszN NV3EXVNDOjRiaB?= M{\2d4Rm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl MV6yOVAzQDR4OR?=
LPS141 M{ixSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXixb4V5Oy5|MzFOwG0> NEjQVpMzPCCq MoHU[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= MV2yOVAzQDR4OR?=
IMR5 NUWxdld3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HMW|I1KGh? NH;LfpRFVVOR M{HEfmlEPTB;MUK2JI5O NUXUSYk5OjRyNEWxO|k>
BE2C M3nW[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjZZlIzPCCq NFfTeGVFVVOR MYLJR|UxRTF|NDDuUS=> MYGyOFA1PTF5OR?=
1643 M1LiO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXOyOEBp M13he2ROW09? NYiwVoVyUUN3ME2xOFchdk1? NGXJXHkzPDB2NUG3PS=>
SKNSH M1zIfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXGNlQhcA>? NFq3TlFFVVOR M1rBOmlEPTB;MUS4JI5O M4X2VVI1ODR3MUe5
SY5Y NIHDS|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HHdlI1KGh? MXnEUXNQ NGG1eVhKSzVyPUG1OEBvVQ>? NInZRpMzPDB2NUG3PS=>
NGP NETpO5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXyyOEBp M3flcmROW09? M{P1bGlEPTB;MUe1JI5O MXWyOFA1PTF5OR?=
KELLY NIjweplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU[yOEBp NVfMSHBWTE2VTx?= MkHETWM2OD1{MkCgcm0> M1m5VVI1ODR3MUe5
CHP134 NFXLSZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTSNlQhcA>? MXXEUXNQ NV;MV4ZwUUN3ME2yO|Mhdk1? MUWyOFA1PTF5OR?=
NLF NUntNWlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXT1UHM5OjRiaB?= NGGxU4ZFVVOR M3fjN2lEPTB;M{K4JI5O M4\ie|I1ODR3MUe5
LAN5 NH3PflVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\JXI5jOjRiaB?= NGfjfplFVVOR MlS3TWM2OD12Mkmgcm0> NX;V[Yx6OjRyNEWxO|k>
NB69 NU\FdlJPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\CNlQhcA>? NVH5OmRjTE2VTx?= MU\JR|UxRTd|ODDuUS=> MXuyOFA1PTF5OR?=
SKNDZ MnjBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVeyOEBp MX;EUXNQ MUXJR|UxRThyMTDuUS=> NWXpfmR3OjRyNEWxO|k>
NBSD NFrhboNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\zNlQhcA>? NHT3cJNFVVOR MUnJR|UxRTF7MECgcm0> NGi4ZZYzPDB2NUG3PS=>
SKNF1 M3LhV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;qXm0zPCCq MlrrSG1UVw>? NIfBWmlKSzVyPUO1NFAhdk1? NF7SWGwzPDB2NUG3PS=>
EBC1 M1fnO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVqyOEBp M1G5SmROW09? M1H5OGlEPTB;NkSwNEBvVQ>? MVGyOFA1PTF5OR?=
SKNAS MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEf3c3MzPCCq Mn7rSG1UVw>? NGnUVmpKSzVy78{eNVAxODBibl2= MoL2NlQxPDVzN{m=
NB16 Mk\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWqzVm9iOjRiaB?= NIGzZoZFVVOR MoXkTWM2OO,:nkGwNFAxKG6P NULyeFBVOjRyNEWxO|k>
RPE1 M3\2eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPSSmMzPCCq NFH2S45FVVOR MY\JR|Ux97zgMUCwNFAhdk1? MYKyOFA1PTF5OR?=

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
NCT02941926 Recruiting Breast Cancer Novartis Pharmaceuticals|Novartis November 30, 2016 Phase 3
NCT02388620 Completed Normal Hepatic Function|Impaired Hepatic Function Novartis Pharmaceuticals|Novartis March 25, 2015 Phase 1
NCT01872260 Recruiting Breast Cancer Novartis Pharmaceuticals|Novartis October 22, 2013 Phase 1
NCT01237236 Active, not recruiting Advanced Solid Tumor|Lymphomas Novartis Pharmaceuticals|Novartis December 21, 2010 Phase 1
NCT03008408 Not yet recruiting Malignant Neoplasms of Female Genital Organs|Endometrial Carcinoma M.D. Anderson Cancer Center|Novartis April 2017 Phase 2
NCT02754011 Recruiting Breast Cancer UNICANCER|Novartis January 2017 Phase 1

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