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 NGPPeoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\JRZozPCCq Ml\4S2k2OD1{N{[gcm0> NYXZd2RlOjV6NUKwOVg>
Myoblast MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7aO|IhcA>? M4DyTmlEPTB;MUCzOUBvVQ>? NVjWOVhVOjV6MUCzO|U>
IMRS NWjkXGU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfKbFk4OiCq NEfteXhKSzVyPUi3N{BvVQ>? M3vpV|I2QDFyM{e1
SKNAS NG\oV4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXq3NkBp M1zIb2lEPTExvK6xNFAxOCCwTR?= NG\ufowzPThzMEO3OS=>
Rh28 M2DGUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYC3NkBp NIXIOYxKSzVyPUi0OUBvVQ>? MkXhNlU5OTB|N{W=
Rh41 MmfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\rO|IhcA>? NYjqXFVFUUN3ME23NVg4KG6P NI\1ZWgzPThzMEO3OS=>
CW9019 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fyfVczKGh? NF7OSFRKSzVyPUm5NVIhdk1? M3H6[FI2QDFyM{e1
Rh5 NI\sc2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\jSWkxPzJiaB?= NUXOe2FnUUN3MP-8olExODByIH7N MlHUNlU5OTB|N{W=
Rh30 NWG3VlI4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWC3NkBp M{n1VWlEPTExvK6xNFAxOCCwTR?= NHT2c3IzPThzMEO3OS=>
778 M1LGN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXewUlRGPzJiaB?= M4Hn[4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> M3fTRVI2ODJ6NE[5
449 Ml;jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2D3TlczKGh? NX\yd4oxcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NH\sb5YzPTB{OES2PS=>
LP3 Mo[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml31O|IhcA>? NWr2[G4{cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M4HDW|I2ODJ6NE[5
LP6 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rRXlczKGh? MnLRbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M2LWUVI2ODJ6NE[5
LP8 NHHMfWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nCZVczKGh? NUXT[YVjcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MmTtNlUxOjh2Nkm=
LPS141 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDkN|U4OiCq NELBTIFqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NFvYdI0zPTB{OES2PS=>
778 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHG1OYY{NjN|IN88US=> MUmyOEBp M4LpeYRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl NXfie|gxOjVyMki0Olk>
449 MmXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DSPVMvOzNizszN M321SlI1KGh? NGrsSWRl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> NGC3XmczPTB{OES2PS=>
LP3 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTTN{4{OyEQvF2= NITMTFIzPCCq M3TR[4Rm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl MknFNlUxOjh2Nkm=
LP6 NXnaVWVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLkN{4{OyEQvF2= NX;6TmI5OjRiaB?= M{ixPIRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl NYXmdopZOjVyMki0Olk>
LP8 M1Hpc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fsZVMvOzNizszN NYfyPZBpOjRiaB?= MoLH[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= M4PqbFI2ODJ6NE[5
LPS141 MorhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\zXVMvOzNizszN MXyyOEBp NVPRdZpH\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> NIL3RW4zPTB{OES2PS=>
IMR5 M2rHVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Moq5NlQhcA>? M3\RWWROW09? M1;Tc2lEPTB;MUK2JI5O MofaNlQxPDVzN{m=
BE2C MnO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPLR2tmOjRiaB?= MWLEUXNQ NXjSfVh3UUN3ME2xN|Qhdk1? MYeyOFA1PTF5OR?=
1643 NIHV[XhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDPNlQhcA>? MnjYSG1UVw>? MXzJR|UxRTF2NzDuUS=> MVuyOFA1PTF5OR?=
SKNSH NF\PdoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVGyOEBp NUewRpdQTE2VTx?= M33Hd2lEPTB;MUS4JI5O M1TINlI1ODR3MUe5
SY5Y MnjtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVuyOEBp MmjHSG1UVw>? NFS0[GNKSzVyPUG1OEBvVQ>? M3TsSlI1ODR3MUe5
NGP NHfF[4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLVT2UzPCCq M1\5N2ROW09? NV;SPWZLUUN3ME2xO|Uhdk1? MWeyOFA1PTF5OR?=
KELLY M1HBdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXSyOEBp MmniSG1UVw>? NEftblJKSzVyPUKyNEBvVQ>? MnOwNlQxPDVzN{m=
CHP134 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnNNlQhcA>? NGXYSJpFVVOR NFfkOolKSzVyPUK3N{BvVQ>? NVPwbY4{OjRyNEWxO|k>
NLF MnnVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3sNlQhcA>? M1fvW2ROW09? NGTTW4FKSzVyPUOyPEBvVQ>? MWKyOFA1PTF5OR?=
LAN5 NVLBcmU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\HT3gzPCCq MV;EUXNQ MWPJR|UxRTR{OTDuUS=> MoDyNlQxPDVzN{m=
NB69 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkG1NlQhcA>? MUHEUXNQ MYXJR|UxRTd|ODDuUS=> NV\TVmp[OjRyNEWxO|k>
SKNDZ NEXoS|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrHZ4FCOjRiaB?= Ml[xSG1UVw>? NGHDcXBKSzVyPUiwNUBvVQ>? M{DwZVI1ODR3MUe5
NBSD NGfhbFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXwWVYzPCCq MUXEUXNQ MoLpTWM2OD1zOUCwJI5O NHvr[IYzPDB2NUG3PS=>
SKNF1 NF3Y[4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHB[pNpOjRiaB?= MV\EUXNQ MnrUTWM2OD1|NUCwJI5O MkH3NlQxPDVzN{m=
EBC1 NEnTe5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTHNlQhcA>? MmDrSG1UVw>? NGXaZlJKSzVyPU[0NFAhdk1? MYSyOFA1PTF5OR?=
SKNAS MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3P0UVI1KGh? NX\uNGg{TE2VTx?= NWrWSFM5UUN3MP-8olExODByIH7N MVeyOFA1PTF5OR?=
NB16 NHHWc|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzOSI0zPCCq NVXGZVNjTE2VTx?= M3npWmlEPTExvK6xNFAxOCCwTR?= MX2yOFA1PTF5OR?=
RPE1 M{fWXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvNdnozPCCq M3\DVWROW09? MUnJR|Ux97zgMUCwNFAhdk1? NEXrVnozPDB2NUG3PS=>

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
NCT02657343 Recruiting Breast Cancer Dana-Farber Cancer Institute|Novartis March 9 2016 Phase 1|Phase 2
NCT02422615 Active not recruiting Breast Neoplasms|Breast Diseases|Neoplasms|Neoplasms by Site|Fulvestrant|Antineoplastic Agents|Antineoplastic Agents Hormonal|Estrogen Receptor Antagonists|Hormone Antagonists|Hormones Hormone Substitutes and Hormone Antagonists|Molecular Mechanisms of Pharmacological Action|Pharmacologic Actions|Therapeutic Use Novartis Pharmaceuticals|Novartis June 9 2015 Phase 3
NCT03114527 Recruiting Soft Tissue Sarcoma Fox Chase Cancer Center August 8 2017 Phase 2
NCT02657928 Active not recruiting Estrogen Receptor Positive|Postmenopausal|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Recurrent Uterine Corpus Carcinoma Mayo Clinic|National Cancer Institute (NCI) July 8 2016 Phase 2
NCT01857193 Active not recruiting Breast Cancer Novartis Pharmaceuticals|Novartis September 6 2013 Phase 1
NCT03434262 Recruiting Anaplastic Astrocytoma|Anaplastic Ependymoma|Anaplastic Ganglioglioma|Anaplastic Meningioma|Anaplastic Oligodendroglioma|Pleomorphic Xanthoastrocytoma Anaplastic|Atypical Teratoid/Rhabdoid Tumor|Brain Cancer|Brain Tumor|Central Nervous System Neoplasms|Choroid Plexus Carcinoma|CNS Embryonal Tumor With Rhabdoid Features|Ganglioneuroblastoma of Central Nervous System|CNS Tumor|Embryonal Tumor of CNS|Ependymoma|Glioblastoma|Glioma|Glioma Malignant|Medulloblastoma|Medulloblastoma; Unspecified Site|Medulloepithelioma|Neuroepithelial Tumor|Neoplasms|Neoplasms Neuroepithelial|Papillary Tumor of the Pineal Region (High-grade Only)|Pediatric Brain Tumor|Pineal Parenchymal Tumor of Intermediate Differentiation (High-grade Only)|Pineoblastoma|Primitive Neuroectodermal Tumor|Recurrent Medulloblastoma|Refractory Brain Tumor|Neuroblastoma. CNS|Glioblastoma IDH-mutant|Glioblastoma IDH-wildtype|Medulloblastoma Group 3|Medulloblastoma Group 4|Glioma High Grade|Neuroepithelial Tumor High Grade|Medulloblastoma SHH-activated and TP53 Mutant|Medulloblastoma SHH-activated and TP53 Wildtype|Medulloblastoma Chromosome 9q Loss|Medulloblastoma Non-WNT Non-SHH NOS|Medulloblastoma Non-WNT/Non-SHH|Medulloblastoma PTCH1 Mutation|Medulloblastoma WNT-activated|Ependymoma Recurrent|Glioma Recurrent High Grade|Glioma Recurrent Malignant|Embryonal Tumor NOS|Glioma Diffuse Midline H3K27M-mutant|Embryonal Tumor With Multilayered Rosettes (ETMR)|Ependymoma NOS WHO Grade III|Ependymoma NOS WHO Grade II|Medulloblastoma G3/G4|Ependymoma RELA Fusion Positive St. Jude Children''s Research Hospital|Novartis Pharmaceuticals March 5 2018 Phase 1

技術サポート

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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

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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
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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