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 34700
JPY 51300
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バルク問合せ

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.

  • 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.

  • 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.

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 M2PXR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDqNlQhcA>? M2H3fGdKPTB;Mke2JI5O NWO3e|hPOjV6NUKwOVg>
Myoblast M2T5V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrURmxlPzJiaB?= NWf1[W5zUUN3ME2xNFM2KG6P MkTINlU5OTB|N{W=
IMRS NVzXTIJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1m1Z|czKGh? NFrLWWhKSzVyPUi3N{BvVQ>? Mn[yNlU5OTB|N{W=
SKNAS NXzkeYs5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWC3NkBp MXnJR|Ux97zgMUCwNFAhdk1? M3PYflI2QDFyM{e1
Rh28 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\Rems5PzJiaB?= NEDBZYJKSzVyPUi0OUBvVQ>? M{jzflI2QDFyM{e1
Rh41 M3j3NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HiTFczKGh? NEi1[ZNKSzVyPUexPFchdk1? NWry[G4zOjV6MUCzO|U>
CW9019 NXvrUY5XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELnUpc4OiCq MYDJR|UxRTl7MUKgcm0> Mny1NlU5OTB|N{W=
Rh5 MoPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorTO|IhcA>? MYfJR|Ux97zgMUCwNFAhdk1? MnrXNlU5OTB|N{W=
Rh30 Mkn6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4f5N|czKGh? MnHoTWM2OO,:nkGwNFAxKG6P MnnlNlU5OTB|N{W=
778 MoXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\MXZFRPzJiaB?= MXLpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NYL2O29IOjVyMki0Olk>
449 Mn\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrnZpExPzJiaB?= NGixOppqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NEGwSXIzPTB{OES2PS=>
LP3 M3;uV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nnTFczKGh? MmfubY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> NILFNnkzPTB{OES2PS=>
LP6 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofvO|IhcA>? M1y3dolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NXnpboZqOjVyMki0Olk>
LP8 M3XhOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIT6fpE4OiCq M2TyO4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> M2XmXVI2ODJ6NE[5
LPS141 MojWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3KVItFPzJiaB?= NWK4cWFMcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MoHjNlUxOjh2Nkm=
778 M3\vVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jBS|MvOzNizszN M1;4c|I1KGh? NV23cHNr\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> M2K0TFI2ODJ6NE[5
449 M1ewfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjRN{4{OyEQvF2= Mmi4NlQhcA>? NH\q[oNl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> MW[yOVAzQDR4OR?=
LP3 NUXUdXc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mln3N{4{OyEQvF2= NX7VfYNrOjRiaB?= M2TEWoRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl NIDpem8zPTB{OES2PS=>
LP6 NXLHcmdUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zVS|MvOzNizszN NUe3bZFbOjRiaB?= MoXZ[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= MX6yOVAzQDR4OR?=
LP8 MorBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVuzMlM{KM7:TR?= MorvNlQhcA>? M1PpVYRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl M3HqVFI2ODJ6NE[5
LPS141 M{jYRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUL5d4x6Oy5|MzFOwG0> NULROJEyOjRiaB?= M4juc4Rm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl MnPoNlUxOjh2Nkm=
IMR5 MmTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHnVWozPCCq MXPEUXNQ NFHXNHJKSzVyPUGyOkBvVQ>? MXiyOFA1PTF5OR?=
BE2C NF\rZotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY[yOEBp Mm\GSG1UVw>? M2\t[WlEPTB;MUO0JI5O NHmwbm0zPDB2NUG3PS=>
1643 M{LPc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LzWlI1KGh? NYfMXXBpTE2VTx?= MVjJR|UxRTF2NzDuUS=> MVyyOFA1PTF5OR?=
SKNSH MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUCyOEBp NUOzSopRTE2VTx?= M3XnbGlEPTB;MUS4JI5O M4XxXlI1ODR3MUe5
SY5Y MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkG2NlQhcA>? NFTX[YxFVVOR M3L0cmlEPTB;MUW0JI5O M33hSlI1ODR3MUe5
NGP M4HaeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\HNlQhcA>? MkLaSG1UVw>? NXn3Z|QxUUN3ME2xO|Uhdk1? MViyOFA1PTF5OR?=
KELLY M3;0Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTnNlQhcA>? M2ruXmROW09? MWrJR|UxRTJ{MDDuUS=> M2jrXFI1ODR3MUe5
CHP134 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVeyOEBp M4DCT2ROW09? NVOxeHNMUUN3ME2yO|Mhdk1? M2nSN|I1ODR3MUe5
NLF NH\POmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTYNlQhcA>? MV7EUXNQ MUnJR|UxRTN{ODDuUS=> NVXUVmRJOjRyNEWxO|k>
LAN5 NXLtRWlOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmT2NlQhcA>? NYG4d5NvTE2VTx?= MlHsTWM2OD12Mkmgcm0> M4G4T|I1ODR3MUe5
NB69 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWmyOEBp NX\0d2JNTE2VTx?= NFjuU3pKSzVyPUezPEBvVQ>? NYDRdIxKOjRyNEWxO|k>
SKNDZ NE\tRXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUiyOEBp NEG4WoNFVVOR NHTDd4NKSzVyPUiwNUBvVQ>? MlfKNlQxPDVzN{m=
NBSD M173Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDiNlQhcA>? M{P3cWROW09? NIflSoxKSzVyPUG5NFAhdk1? NFzySoszPDB2NUG3PS=>
SKNF1 MmXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjmVmRxOjRiaB?= M{LoUGROW09? MYDJR|UxRTN3MECgcm0> MlLMNlQxPDVzN{m=
EBC1 MoP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPkZ5gzPCCq MWPEUXNQ MYrJR|UxRTZ2MECgcm0> NWG1d2hzOjRyNEWxO|k>
SKNAS NHXpcpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjXR2NbOjRiaB?= M1OwUWROW09? M{HENGlEPTExvK6xNFAxOCCwTR?= NFPKO48zPDB2NUG3PS=>
NB16 NGTWNWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFz3Z4YzPCCq NH;tRXBFVVOR M2O2e2lEPTExvK6xNFAxOCCwTR?= MUGyOFA1PTF5OR?=
RPE1 M3z0S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\2NlQhcA>? M3TKfWROW09? MVzJR|Ux97zgMUCwNFAhdk1? M1XZelI1ODR3MUe5

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]

+ 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
NCT03834740 Recruiting 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 Recruiting Early Breast Cancer Novartis Pharmaceuticals|Translational Research in Oncology|Novartis December 7 2018 Phase 3
NCT03613220 Recruiting 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

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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