Ribociclib (LEE011)

For research use only. Not for use in humans.

製品コードS7440

Ribociclib (LEE011)化学構造

CAS No. 1211441-98-3

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

サイズ 価格(税別)  
JPY 34700
JPY 51300
JPY 86960
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バルク問合せ

文献中Selleckの製品使用例(54)

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 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
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NCI-H1299 NH75eY9EgXSxdH;4bYNqfHliYYPzZZk> MXG3NkBpenN? NILUXmZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBPS0lvSEGyPVkh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGGodHXyJFczKGi{czDifUBES0t6IHHzd4F6NCCLQ{WwJF0hPS52NjFOwG0v M3;kNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUG4N|EzLz5{OUWxPFMyOjxxYU6=
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T47D Mnz4R5l1d3SxeHnjbZR6KGG|c3H5 NFnPNng4OiCqcoO= M1;HcGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHQ1P0RiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSCFQ1u4JIF{e2G7LDDJR|UxKD1iNj6yN{DPxE1w NEfRU|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWxPFMyOid-Mkm1NVg{OTJ:L3G+
H1299 MmnnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1LQZVczKGi{cx?= M2HyRWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGgyOjl7IHPlcIx{KGmwY4XiZZRm\CCob4KgO|IhcHK|IHL5JGNEUzhiYYPzZZktKEmFNUCgQUA4NjZ|NzFOwG0v NYfVPIVrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2OVE6PzlpPkK4OlUyQTd7PD;hQi=>
KOPN8 MkHTRZBweHSxc3nzJIF{e2G7 NUW4eFZGOC53IIXN NFfwdnA{KGi{cx?= Ml7vTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCNT2DOPEBk\WyuczDhd5Nme3OnZDDhd{B2eHKnZ4XsZZRqd25ib3[gZ4xm[X[nZDDQRXJRKGyndnXsJIF1KDBwNTD1UUBi\nSncjCzJIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> M1y0N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEC3PVc2Lz5{OUSwO|k4PTxxYU6=
KOPN8 M3u5UGFxd3C2b4Ppd{Bie3OjeR?= NIjic3QxNjVidV2= NWjHZZo3OjRiaILz MkDwTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCNT2DOPEBk\WyuczDhd5Nme3OnZDDhd{B2eHKnZ4XsZZRqd25ib3[gZ4xm[X[nZDDQRXJRKGyndnXsJIF1KDBwNTD1UUBxemVvdILlZZRm\CC5aYToJG5CSyCob4KgNUBpeiCjbnSgcYVie3W{ZXSgZYZ1\XJiMkSgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> NUfR[4tpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0NFc6PzVpPkK5OFA4QTd3PD;hQi=>
Hep3B M2nlfmNmdGxiY4njcIUh[XO|YYm= MWiyOEBpenN? NVvSOFNPS2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hUGWyM1KgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IFewM2cyKHCqYYPlJIFnfGW{IEK0JIhzeyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pIHLhd4VlKG[ub4egZ5l1d22ndIL5 NFXHN3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWxPFMyOid-Mkm1NVg{OTJ:L3G+
HepG2 MX7D[YxtKGO7Y3zlJIF{e2G7 MmfCNlQhcHK| M4[0V2NmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJGhmeEd{IHPlcIx{KGG|c3Xzd4VlKGG|IHHjZ5VufWyjdHnvckBifCCJMD;HNUBxcGG|ZTDh[pRmeiB{NDDodpMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\yCkYYPl[EBndG:5IHP5eI9u\XS{eR?= NXL4SmhPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NVg{OTJpPkK5OVE5OzF{PD;hQi=>
A549 M122[2NmdGxiY4njcIUh[XO|YYm= MkLENlQhcHK| M2\XcmNmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJGE2PDliY3XscJMh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJIF1KEdyL1exJJBp[XOnIHHmeIVzKDJ2IHjyd{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oKGKjc3XkJIZtd3diY4n0c41mfHK7 M{HIV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUG4N|EzLz5{OUWxPFMyOjxxYU6=
NCI-H460 MlTzR4VtdCCleXPs[UBie3OjeR?= MlPGNlQhcHK| MU\D[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDOR2kuUDR4MDDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{CvS|EheGijc3WgZYZ1\XJiMkSgbJJ{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdiYnHz[YQh\myxdzDjfZRwdWW2com= NU\vUZVRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NVg{OTJpPkK5OVE5OzF{PD;hQi=>
T47D MWDD[YxtKGO7Y3zlJIF{e2G7 Ml\XNlQhcHK| MlLUR4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gWFQ4TCClZXzsd{Bie3Onc4Pl[EBieyCjY3P1cZVt[XSrb36gZZQhTzBxR{GgdIhie2ViYX\0[ZIhOjRiaILzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcoch[mG|ZXSg[oxwfyCleYTvcYV1enl? M4rj[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUG4N|EzLz5{OUWxPFMyOjxxYU6=
MDA-MB-231 MXfD[YxtKGO7Y3zlJIF{e2G7 MlPBNlQhcHK| M3TR[2NmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZZN{\XO|ZXSgZZMh[WOldX31cIF1cW:wIHH0JGcxN0dzIIDoZZNmKGGodHXyJFI1KGi{czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nJIJie2WmIH\sc5ch[3m2b33leJJ6 NUfVO3U{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NVg{OTJpPkK5OVE5OzF{PD;hQi=>
Fluc-labeled 4T1 NGTLcZFCdnSrdIXtc5Ih[XO|YYm= Mn\INVMxKG2pL3vn Mmq3NVgh\GG7cx?= NXzmbINySW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhdW:3c3WgSox2[y2uYXLlcIVlKDSWMTDj[YxteyCrbYDsZY51\WRiaX6gRoFt[i:lIH3veZNmKGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckB1fW2xcjD3[YlocHRiYYSgNVMxKG2pL3vnMEBqeCCjZH3pcol{fGW{ZXSg[IFqdHliZn;yJFE5KGSjeYOgcYVie3W{ZXSgZYZ1\XJiODD0c{AzPSCmYYnz NV3MTY4xRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NVg{OTJpPkK5OVE5OzF{PD;hQi=>
T47D M1PRW2NmdGxiY4njcIUh[XO|YYm= NIe0S20zPCCqcoO= MkDRTY5lfWO2aX;uJI9nKGOnbHygZ5lkdGViYYLy[ZN1KGmwIHj1cYFvKFR2N1SgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4hTzBxR{GgdIhie2ViYXPjeY12dGG2aX;uJIlv[3WkYYTl[EBnd3JiMkSgbJJ{KGK7IH\sc5ch[3m2b33leJJ6 NFi2fmY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[1NVk4QSd-Mki2OVE6Pzl:L3G+

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

アッセイ
Methods Test Index PMID
Western blot
pRb(S807) / Rb / p53 / Cyclin E / Cyclin D1 / CDK4 / CDK6 / p27 / p21 / PARP; 

PubMed: 29789630     


Effect of ribociclib on pRB and G1 cell cycle regulating protein expressions in C666-1 and HK1 cells. Cells were treated with ribociclib in 2 concentrations, one of them near their corresponding IC50, for 24 and 48 hours. Phosphorylation of Rb in all cell䲧疝Ỵ疞㧀疜膉痘 瘿뾠ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ՂĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ⟸෕䐺痖暼瘿⟸෕ᾰƌ ⟸෕Ð㺣痖⟸෕€𢡄⟼෕€䀷痗⟼෕౴⟼෕

29789630
Growth inhibition assay
Cell viability ; 

PubMed: 26390342     


Effects of palbociclib and ribociclib on viability of H157, H2170, H520 and H596 cells after 72 hours of drug treatment and IC50 values for inhibition of 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]

- 合併
  • 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]

- 合併
  • 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.
    (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
Storage powder
in solvent
別名 N/A
Smiles CN(C)C(=O)C1=CC2=CN=C(N=C2N1C3CCCC3)NC4=NC=C(C=C4)N5CCNCC5

投与溶媒組成計算器(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)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
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
計算リセット

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 (mg) = 濃度 (mM) x 体積 (mL) 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 interventions Conditions Sponsor/Collaborators Start Date Phases
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) March 2021 --
NCT04315233 Recruiting Drug: Ribociclib|Drug: Belinostat Metastatic Breast Cancer|Recurrent Ovarian Carcinoma University of Utah|Novartis|Acrotech Biopharma October 29 2020 Phase 1
NCT03834740 Recruiting Drug: Ribociclib|Drug: Everolimus Glioblastoma Multiforme|Glioma of Brain St. Joseph''s Hospital and Medical Center Phoenix|Ivy Brain Tumor Center|Barrow Neurological Institute December 21 2018 Early Phase 1
NCT03701334 Active not recruiting Drug: Ribociclib|Other: Endocrine Therapy Early Breast Cancer Novartis Pharmaceuticals|Translational Research in Oncology|Novartis December 7 2018 Phase 3
NCT03613220 Completed Drug: ribociclib|Drug: letrozole HR+ HER2 Breast Cancer Novartis Pharmaceuticals|Novartis December 28 2018 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

相関CDK製品

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
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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