Ceritinib (LDK378)

For research use only. Not for use in humans.

製品コードS7083

Ceritinib (LDK378)化学構造

CAS No. 1032900-25-6

Ceritinib (LDK378) is potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays. Ceritinib (LDK378) also inhibits IGF-1R, InsR, STK22D and FLT3 with IC50 of 8 nM, 7 nM, 23 nM and 60 nM, respectively. Phase 3.

サイズ 価格(税別) 在庫  
JPY 26400 あり
JPY 80000 あり
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バルク問合せ

文献中Selleckの製品使用例(60)

製品安全説明書

ALK阻害剤の選択性比較

生物活性

製品説明 Ceritinib (LDK378) is potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays. Ceritinib (LDK378) also inhibits IGF-1R, InsR, STK22D and FLT3 with IC50 of 8 nM, 7 nM, 23 nM and 60 nM, respectively. Phase 3.
特性 Does not cross react with c-Met, and has an improved in vivo glucose homeostasis profile relative to TAE684. May be active in Crizotinib-relapsed tumors.
ターゲット
ALK [1]
(Cell-free assay)
Insulin Receptor [1]
(Cell-free assay)
IGF-1R [1]
(Cell-free assay)
STK22D [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
0.2 nM 7 nM 8 nM 23 nM 60 nM
体外試験

LDK378 shows great anti-proliferative activity in Ba/F3-NPM-ALK and Karpas290 cells with IC50 of 26.0 nM and 22.8 nM, compared with IC50 of 319.5 nM and 2477 nM in Ba/F3-Tel-InsR and Ba/F3-WT cells. [1]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Parental(+IL3) NYDP[YFKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1n3WFczKGh? MXTEUXNQ MV;JR|UxRTF3OE[gxtEhOTd|IH7N NWi2OFZsOjV5NEmwN|Q>
WT 70 NWn2XodrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTiU2I4OiCq MontSG1UVw>? M13nZWlEPTB;MkGgxtEhQCCwTR?= M33vWlI2PzR7MEO0
G1128S 1022 NUPZTo51T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXO3NkBp NYryVVFkTE2VTx?= NV7tTFRvUUN3ME2xNFIhyrFiM{igcm0> MXKyOVc1QTB|NB?=
C1156F 1293 MoDqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1mzSFczKGh? NUf6UVkyTE2VTx?= M2\0XGlEPTB;MkG3JOKyKDFzNTDuUS=> M1XUZVI2PzR7MEO0
I1171N 519 MkfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDqNJY4OiCq MWnEUXNQ M{XzVGlEPTB;MUi3JOKyKDh5IH7N NIPTXo4zPTd2OUCzOC=>
I1171T 445 M33IOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfv[|RwPzJiaB?= NVrvbnZoTE2VTx?= M4LzOmlEPTB;OEKgxtEhOTJibl2= NFTXfoUzPTd2OUCzOC=>
F1174I 184 MmjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\KUIc4OiCq NInWWplFVVOR MYPJR|UxRTF|INMxJFAvOSCwTR?= M1rEdlI2PzR7MEO0
N1178H 169 Mme1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoezO|IhcA>? MX3EUXNQ NG\TRppKSzVyPUSyJOKyKDZibl2= NH\KbXkzPTd2OUCzOC=>
E1210K 748 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4[zSVczKGh? MVvEUXNQ NIjuNppKSzVyPUG4O{DDuSB6NDDuUS=> MWGyOVc1QTB|NB?=
C1156F/D1203N 2809 MkHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEO1Rmk4OiCq M1W5RWROW09? NF7NR4hKSzVyPUK1OEDDuSB7OTDuUS=> NXjq[5g4OjV5NEmwN|Q>
Ba/F3 NA WT MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV63NkBp Mk[zTWM2OD1yLkCyNEDPxE1? NUewVWF1OjV5Mke0NFA>
Ba/F3 NA C1156Y Mn3tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk[xO|IhcA>? MWnJR|UxRTBwMEexJO69VQ>? MVqyOVczPzRyMB?=
Ba/F3 NA L1196M NFHrcI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLQXVRHPzJiaB?= Ml7STWM2OD1yLkC0NkDPxE1? NXHHNoZPOjV5Mke0NFA>
Ba/F3 NA L1152R M2W4c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2r0XVczKGh? M3\jV2lEPTB;MD6yPFgh|ryP NFvOO2UzPTd{N{SwNC=>
Ba/F3 NA G1202R NYXSUWN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFv6fZQ4OiCq NVi4[ZE4UUN3ME2wMlI4PyEQvF2= M33KTFI2PzJ5NECw
Ba/F3 NA G1269A M1rPWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfCTnM4OiCq M3;wc2lEPTB;MD6wNVkh|ryP M{LUPVI2PzJ5NECw
Ba/F3 NA S1206Y NY\jVWxNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWK3NkBp M2Hld2lEPTB;MD6wN|ch|ryP NU\BUIhkOjV5Mke0NFA>
Ba/F3 EA WT NFG3UpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVm3NkBp MXLJR|UxRTBwMEKxJO69VQ>? NH\SWXEzPTd{N{SwNC=>
Ba/F3 EA C1156Y Mk\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTWdHc4OiCq NUnpWYtYUUN3ME2wMlAzPiEQvF2= MUSyOVczPzRyMB?=
Ba/F3 EA L1196M MkDnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVi3NkBp NYr1[HRyUUN3ME2wMlAyQSEQvF2= NXfjXG5WOjV5Mke0NFA>
Ba/F3 EA L1152R MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV:3NkBp MlznTWM2OD1yLkC5PUDPxE1? NVL4XpBSOjV5Mke0NFA>
Ba/F3 EA G1202R MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjwTXc4OiCq NEDaVFZKSzVyPUCuOFY4KM7:TR?= MXKyOVczPzRyMB?=
Ba/F3 EA G1269A MmfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXy3NkBp MVfJR|UxRTBwMEOzJO69VQ>? MVGyOVczPzRyMB?=
Ba/F3 EA S1206Y M1XYeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7NO|IhcA>? M2PocmlEPTB;MD6wN|gh|ryP NFzwb3ozPTd{N{SwNC=>

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アッセイ
Methods Test Index PMID
Western blot
p-ALK / ALK / p-AKT / AKT / p-ERK / ERK; 

PubMed: 28425916     


Inhibition of ALK autophosphorylation and downstream signaling by ceritinib, crizotinib and PF06463922 in NB-1 cells. Cells were harvested after treatment for 4 hr with the indicated compounds at different concentrations. Whole cell lysates were analyzed by Western blotting to detect the levels of ALK, AKT and ERK proteins and their phosphorylation.

pROS1 / ROS1 / pSTAT3 / STAT3 ; 

PubMed: 25351743     


Inhibition of phospho-ROS1 by various ALK inhibitors in Ba/F3 models. CD74-ROS1 expressing Ba/F3 cells were exposed to increasing concentrations of crizotinib, ceritinib, AP26113, or ASP3026 for 3 h. Cell lysates were immunoblotted to detect the indicated proteins.

28425916 25351743
Growth inhibition assay
Cell viability; 

PubMed: 29067644     


The effects of ceritinib treatment on cell viability in ARMS and ERMS cell lines. Cells were treated with 0-5 μM ceritinib for 72 h (Rh30, RD), 120 h (Rh41), or 144 h (Rh18, Aska) and cell viability was assessed. The y-axis represents relative cell viability compared to non-treated cells (control). Effects on cell viability were determined in triplicate. Values are presented as mean ± SD. Dotted line represents the IC50-value. The human synovial sarcoma cell line Aska with constitutive ALK phosphorylation was used as a positive control.

29067644
体内試験 LDK378 is designed to reduce the possibility of forming reactive metabolites and shows undetectable levels of glutathione (GSH) adducts (<1%) in liver microsomes. LDK378 has relatively good metabolic stability, with moderate CYP3A4 (Midazolam substrate) inhibition and hERG inhibition. LDK378 exhibits low plasma clearance in animals (mouse, rat, dog and monkey) compared to liver blood flow, with the oral bioavailability of above 55% in mouse, rat, dog and monkey. LDK378 induces a dose-dependent growth inhibition and tumor regression in the Karpas299 and H2228 rat xenograft models, with no body-weight loss. LDK378 shows no impact on insulin levels or plasma glucose utilization in the mouse upon chronic dosing up to 100 mg/kg. [1]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
- 合併

Enzymatic kinase profiling description:

All kinases are expressed as either Histidine- or GST-tagged fusion proteins using the baculovirus expression technology except for the untagged ERK2 which is produced in E. coli. The kinase activity is measured in the LabChip mobility shift assay. The assay is performed at 30°C for 60 min. The effect of LDK378 on the enzymatic activity is obtained from the linear progress curves in the absence and presence of LDK378 and routinely determines from one reading (end point measurement)
細胞試験: [1]
- 合併
  • 細胞株: Ba/F3-NPM-ALK, Ba/F3-Tel-InsR, Ba/F3-WT, Karpas299 cells
  • 濃度: ~100 μM
  • 反応時間: 2-3 days
  • 実験の流れ: Luciferase-expressing cells are incubated with serial dilutions of LDK378 or DMSO for 2-3 days. Luciferase expression is used as a measure of cell proliferation/survival and is evaluated with the Bright-Glo Luciferase Assay System. IC50 values are generated by using XLFit software.
    (参考用のみ)
動物試験:[1]
- 合併
  • 動物モデル: RNU nude rats bearing the Karpas299/H2228 tumors
  • 投薬量: ~50 mg/kg
  • 投与方法: Oral gavage
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 20 mg/mL (35.83 mM) warming
Water Insoluble
Ethanol '3 mg/mL '3

* 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 558.14
化学式

C28H36ClN5O3S

CAS No. 1032900-25-6
Storage powder
in solvent
別名 N/A
Smiles CC1=CC(=C(C=C1C2CCNCC2)OC(C)C)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)C(C)C)Cl

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
NCT02450903 Completed Drug: LDK378 Non-Small-Cell Lung Cancer Novartis Pharmaceuticals|Novartis August 21 2015 Phase 2
NCT02276027 Completed Drug: BYL719|Drug: INC280|Drug: LDK378|Drug: MEK162 Adenocarcinoma Lung Cancer; Squamous Cell Lung Carcinoma Novartis Pharmaceuticals|Novartis January 20 2015 Phase 2
NCT02040870 Completed Drug: LDK378 Non-Small Cell Lung Cancer Novartis Pharmaceuticals|Novartis March 7 2014 Phase 1|Phase 2
NCT01950481 Completed Drug: LDK378 Normal Hepatic Function|Impaired Hepatic Function Novartis Pharmaceuticals|Novartis January 2014 Phase 1
NCT01772797 Completed Drug: LDK378|Drug: AUY922 Anaplastic Lymphoma Kinase (ALK)|Non-small Cell Lung Cancer Novartis Pharmaceuticals|Novartis June 2013 Phase 1
NCT01685060 Completed Drug: LDK378 Non-Small Cell Lung Cancer Novartis Pharmaceuticals|Novartis November 26 2012 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

よくある質問(FAQ)

  • 質問1:

    how to reconstitute the inhibitor for oral administration to mice?

  • 回答:

    You can resuspend LDK378 in 30% PEG400/0.5% Tween 80/5% propylene glycol and use the suspension for oral gavage feeding.

ALKシグナル伝達経路

ALK Inhibitors with Unique Features

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Tags: Ceritinib (LDK378)を買う | Ceritinib (LDK378) ic50 | Ceritinib (LDK378)供給者 | Ceritinib (LDK378)を購入する | Ceritinib (LDK378)費用 | Ceritinib (LDK378)生産者 | オーダーCeritinib (LDK378) | Ceritinib (LDK378)化学構造 | Ceritinib (LDK378)分子量 | Ceritinib (LDK378)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