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(3)

  • 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 MkfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7GNlQhcA>? MornS2k2OD1{N{[gcm0> MkDJNlU5PTJyNUi=
Myoblast MkjaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXezdHpWPzJiaB?= MUDJR|UxRTFyM{Wgcm0> MYKyOVgyODN5NR?=
IMRS M{fhemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUe3NkBp NX\2dmdFUUN3ME24O|Mhdk1? MU[yOVgyODN5NR?=
SKNAS M2rFU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUO3cm5{PzJiaB?= NWHaW2lWUUN3MP-8olExODByIH7N NIDtWokzPThzMEO3OS=>
Rh28 NYri[lFQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\SO|IhcA>? M{C2fmlEPTB;OES1JI5O MYKyOVgyODN5NR?=
Rh41 MmXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonVO|IhcA>? MUDJR|UxRTdzOEegcm0> NWPzSZdzOjV6MUCzO|U>
CW9019 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnS4O|IhcA>? NYmzZVFtUUN3ME25PVEzKG6P NXzwOmhGOjV6MUCzO|U>
Rh5 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULlOIxRPzJiaB?= MXnJR|Ux97zgMUCwNFAhdk1? NVvYSpY2OjV6MUCzO|U>
Rh30 NGWzc25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEWwb|Y4OiCq NIDCNZBKSzVy78{eNVAxODBibl2= MVmyOVgyODN5NR?=
778 M1WwSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkC3O|IhcA>? MUjpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M2LKTVI2ODJ6NE[5
449 M2fqOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVu3NkBp NWPKUJhQcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MV6yOVAzQDR4OR?=
LP3 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfSU3M4OiCq MmPVbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M3TPSlI2ODJ6NE[5
LP6 M2HCc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HKVFczKGh? M2LwVYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NEnHVGYzPTB{OES2PS=>
LP8 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPXO|IhcA>? NH;ndnlqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 MkHzNlUxOjh2Nkm=
LPS141 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrQSngxPzJiaB?= NVH1[lhwcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NVzTWGFNOjVyMki0Olk>
778 NHfYeYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFq0WVY{NjN|IN88US=> MVuyOEBp NVfV[3lP\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> NUDxPHZ7OjVyMki0Olk>
449 NHXPcIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvjbJM{NjN|IN88US=> MY[yOEBp Mli5[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= MnXnNlUxOjh2Nkm=
LP3 NYXsVo1jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLYN{4{OyEQvF2= NYTzN5k3OjRiaB?= Mn2x[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= NY\5WpdJOjVyMki0Olk>
LP6 M3fzSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXES3AyOy5|MzFOwG0> MlXVNlQhcA>? MoXD[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= NGfrR5AzPTB{OES2PS=>
LP8 M1[4NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWizMlM{KM7:TR?= NFPMZ3IzPCCq NFf4Tpdl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> MnLXNlUxOjh2Nkm=
LPS141 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHRdmY5Oy5|MzFOwG0> MUeyOEBp MY\k[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NV3mZYo4OjVyMki0Olk>
IMR5 M{HDSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjnNlQhcA>? MXLEUXNQ MV7JR|UxRTF{NjDuUS=> M3vYNVI1ODR3MUe5
BE2C NIjxUoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLN[GUzPCCq NYrIS3MzTE2VTx?= MXnJR|UxRTF|NDDuUS=> MWOyOFA1PTF5OR?=
1643 NY\leFV{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfkNlQhcA>? MYrEUXNQ M2LYPWlEPTB;MUS3JI5O NVf4NnVbOjRyNEWxO|k>
SKNSH M13xRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjGNlQhcA>? NWTrVHdDTE2VTx?= M1LUc2lEPTB;MUS4JI5O NUDuVmdVOjRyNEWxO|k>
SY5Y M1yze2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rDW|I1KGh? M3TOdWROW09? MXLJR|UxRTF3NDDuUS=> MX2yOFA1PTF5OR?=
NGP Ml\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTIW3ZyOjRiaB?= MoPFSG1UVw>? NH2xfXNKSzVyPUG3OUBvVQ>? NXXJUm0xOjRyNEWxO|k>
KELLY MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnSVWM1OjRiaB?= NUfISGp1TE2VTx?= NX\BeJFoUUN3ME2yNlAhdk1? NYD1NmdZOjRyNEWxO|k>
CHP134 NHPzOIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXtXYUzPCCq M4HQZWROW09? NFfCb3VKSzVyPUK3N{BvVQ>? NH;5NHgzPDB2NUG3PS=>
NLF NUKwZnBRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWSyOEBp NIfRflZFVVOR NHLkPZRKSzVyPUOyPEBvVQ>? NHLvSWozPDB2NUG3PS=>
LAN5 NFe4T5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnONlQhcA>? NGTNXGRFVVOR Mn;STWM2OD12Mkmgcm0> NYLPOWk6OjRyNEWxO|k>
NB69 NG\oeXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDWbnJuOjRiaB?= NVXyZppQTE2VTx?= MVXJR|UxRTd|ODDuUS=> NFi4dZQzPDB2NUG3PS=>
SKNDZ MkLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLLZYczPCCq NIXxUnJFVVOR NWLoRWpmUUN3ME24NFEhdk1? MXKyOFA1PTF5OR?=
NBSD M3SyOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLPNlQhcA>? NXf2[Xl{TE2VTx?= NH7RcIlKSzVyPUG5NFAhdk1? NWmyOphrOjRyNEWxO|k>
SKNF1 M1K3VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{faelI1KGh? MmPsSG1UVw>? NInPN|FKSzVyPUO1NFAhdk1? M4PXXVI1ODR3MUe5
EBC1 MlPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWSyOEBp MoDMSG1UVw>? NXXBfIhTUUN3ME22OFAxKG6P NFXlNGczPDB2NUG3PS=>
SKNAS NH3VT4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HJ[VI1KGh? M4nLVWROW09? MoTiTWM2OO,:nkGwNFAxKG6P NHPQNHYzPDB2NUG3PS=>
NB16 NUnLd4tJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnP3NlQhcA>? M1nETGROW09? MVrJR|Ux97zgMUCwNFAhdk1? M3P6[lI1ODR3MUe5
RPE1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvlboEzPCCq M33jZmROW09? NHLpVlFKSzVy78{eNVAxODBibl2= M2eyWFI1ODR3MUe5

多くの細胞株試験データを見る場合、クリックしてください

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

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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 ( 輸入 輸出 )

  • 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

マス 濃度 ボリューム 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