Ceritinib (LDK378)

製品コードS7083

Ceritinib (LDK378)化学構造

分子量(MW):558.14

Ceritinib (LDK378) is potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively. Phase 3.

サイズ 価格(税別)  
JPY 24402.00
JPY 78020.00

カスタマーフィードバック(3)

  • Quantitation of crystal violet uptake by ORF-expressing cells exposed to crizotinib (CRZ) or ceritinib (CER) normalized to Lac Z. Mean and SE are shown for six (CRZ) or four (CER) independent experiments of three replicates each.

    Cancer Cell, 2015, 27(3): 397-408 . Ceritinib (LDK378) purchased from Selleck.

    H3122 cells expressing pRS or shSMARCE1 vectors were cultured in the absence or presence of 100 nM NVP-TAE684, 400 nM Ceritinib, 1 μM gefitinib or their combination for 3 h. Cell lysates were harvested for immunoblot analysis and probed for the indicated proteins.

    Cell Res, 2015, 25(4): 445-58. Ceritinib (LDK378) purchased from Selleck.

  • (A) H3122 LDK_R show increased invasive and migratory capabilities compared to parental H3122, (B) loss of E-cadherin and increased mesenchymal markers including vimentin and AXL. Knockdown of vimentin decreased AXL expression in H3122 LDK_R.

    Mol Oncol, 2016, 10(4):601-9. Ceritinib (LDK378) purchased from Selleck.

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, shows 40- and 35-fold selectivity against IGF-1R and InsR, 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)
0.2 nM 7 nM 8 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) NVjoRXVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Lqd|czKGh? MoHCSG1UVw>? MW\JR|UxRTF3OE[gxtEhOTd|IH7N NFfGRXAzPTd2OUCzOC=>
WT 70 Mkf5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mki3O|IhcA>? MWDEUXNQ MVrJR|UxRTJzINMxJFghdk1? MlfXNlU4PDlyM{S=
G1128S 1022 NWTo[XZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmGzO|IhcA>? MkHISG1UVw>? NI\ZO3NKSzVyPUGwNkDDuSB|ODDuUS=> MUiyOVc1QTB|NB?=
C1156F 1293 NYPPfHlXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUT6O5BQPzJiaB?= M2naVmROW09? M2nmU2lEPTB;MkG3JOKyKDFzNTDuUS=> MUSyOVc1QTB|NB?=
I1171N 519 NG[0WoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2X0NFczKGh? NV:3epVmTE2VTx?= NWTzdZJwUUN3ME2xPFchyrFiOEegcm0> NHjvXm8zPTd2OUCzOC=>
I1171T 445 M2\tU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXSboFWPzJiaB?= M4PQTmROW09? MWrJR|UxRTh{INMxJFEzKG6P NVzKZm5ZOjV5NEmwN|Q>
F1174I 184 NI[5W4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUW3NkBp MXXEUXNQ M{ThW2lEPTB;MUOgxtEhOC5zIH7N NE[1SFczPTd2OUCzOC=>
N1178H 169 Mn7KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVywfYduPzJiaB?= MWXEUXNQ M3\GNmlEPTB;NEKgxtEhPiCwTR?= MUeyOVc1QTB|NB?=
E1210K 748 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXW3NkBp MnzoSG1UVw>? NE\hc3JKSzVyPUG4O{DDuSB6NDDuUS=> NHnVeHEzPTd2OUCzOC=>
C1156F/D1203N 2809 NF\j[HZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVS3NkBp MWTEUXNQ MXnJR|UxRTJ3NDFCtUA6QSCwTR?= M1zjeVI2PzR7MEO0
Ba/F3 NA WT NInrXW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jlSlczKGh? M2\VeGlEPTB;MD6wNlAh|ryP MVqyOVczPzRyMB?=
Ba/F3 NA C1156Y NUDROWY3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[zO|IhcA>? NHXJOHdKSzVyPUCuNFcyKM7:TR?= M3nwPFI2PzJ5NECw
Ba/F3 NA L1196M MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrHUppEPzJiaB?= NVnrXZBFUUN3ME2wMlA1OiEQvF2= MUmyOVczPzRyMB?=
Ba/F3 NA L1152R MlTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLuUGhRPzJiaB?= NX;pS4hXUUN3ME2wMlI5QCEQvF2= NGK2c5EzPTd{N{SwNC=>
Ba/F3 NA G1202R MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLLXZBvPzJiaB?= NFXPdoVKSzVyPUCuNlc4KM7:TR?= NXfndGZQOjV5Mke0NFA>
Ba/F3 NA G1269A MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUS3NkBp Mo\TTWM2OD1yLkCxPUDPxE1? NYizdHpOOjV5Mke0NFA>
Ba/F3 NA S1206Y NX\LbZljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUm3NkBp Mn:wTWM2OD1yLkCzO{DPxE1? NEXJWJAzPTd{N{SwNC=>
Ba/F3 EA WT NH[wclZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2CxblczKGh? MYXJR|UxRTBwMEKxJO69VQ>? MlrLNlU4Ojd2MEC=
Ba/F3 EA C1156Y NH3GXYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkizO|IhcA>? MoLSTWM2OD1yLkCyOkDPxE1? M1L0ZVI2PzJ5NECw
Ba/F3 EA L1196M MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGeze2M4OiCq M3f0UmlEPTB;MD6wNVkh|ryP NHvVcmIzPTd{N{SwNC=>
Ba/F3 EA L1152R MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfkO|IhcA>? NED6dJlKSzVyPUCuNFk6KM7:TR?= NYnmO|ZXOjV5Mke0NFA>
Ba/F3 EA G1202R MkCwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHVO|IhcA>? NEfFNIpKSzVyPUCuOFY4KM7:TR?= MVGyOVczPzRyMB?=
Ba/F3 EA G1269A NXrjSW93T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV63NkBp MYTJR|UxRTBwMEOzJO69VQ>? M2L6R|I2PzJ5NECw
Ba/F3 EA S1206Y MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjwO|IhcA>? NEOzWY1KSzVyPUCuNFM5KM7:TR?= MX[yOVczPzRyMB?=

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 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]
+ 展開

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]
+ 展開
  • 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]
+ 展開
  • 動物モデル: RNU nude rats bearing the Karpas299/H2228 tumors
  • 製剤: LDK378 (phosphate salt) formulated in 0.5% methylcellulose/0.5% Tween 80
  • 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
Ethanol 3 mg/mL (5.37 mM)
Water Insoluble

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)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
保管
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
NCT02321501 Recruiting Head and Neck Cancer|Lung Cancer M.D. Anderson Cancer Center|Novartis June 2016 Phase 1
NCT02465528 Recruiting Tumors With Aberrations in ALK Novartis Pharmaceuticals|Novartis March 2016 Phase 2
NCT02450903 Recruiting Non-Small-Cell Lung Cancer Novartis Pharmaceuticals|Novartis August 2015 Phase 2
NCT02393625 Recruiting ALK-positive NSCLC Novartis Pharmaceuticals|Novartis May 2015 Phase 1
NCT02374489 Recruiting Cholangiocarcinoma National Health Research Institutes, Taiwan|National Cheng-Kung University Hospital|National Taiwan University Hospital March 2015 Phase 2
NCT02276027 Recruiting Adenocarcinoma Lung Cancer; Squamous Cell Lung Carcinoma Novartis Pharmaceuticals|Novartis January 2015 Phase 2

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題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.

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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