1. Protein Tyrosine Kinase/RTK
  2. ALK
    Insulin Receptor
    IGF-1R
  3. Ceritinib dihydrochloride

Ceritinib dihydrochloride (Synonyms: LDK378 dihydrochloride)

目录号: HY-15656A 纯度: 99.98%
产品使用指南

Ceritinib dihydrochloride (LDK378 dihydrochloride) 是一种选择性,口服可生物利用且具有 ATP 竞争性的 ALK 酪氨酸激酶抑制剂,IC50 为 200 pM。Ceritinib dihydrochloride (LDK378 dihydrochloride) 还抑制 IGF-1RInsRSTK22DIC50 值分别为 8、7 和 23 nM。Ceritinib dihydrochloride (LDK378 dihydrochloride) 显示出良好的抗肿瘤效力。

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Ceritinib dihydrochloride Chemical Structure

Ceritinib dihydrochloride Chemical Structure

CAS No. : 1380575-43-8

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Size Price Stock Quantity
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥902 In-stock
5 mg ¥650 In-stock
10 mg ¥1000 In-stock
50 mg ¥2500 In-stock
100 mg ¥3500 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of Ceritinib dihydrochloride:

Top Publications Citing Use of Products

    Ceritinib dihydrochloride purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):996-1006.

    Dose-response and time course comparison of ALK inhibition by Crizotinib or Ceritinib.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    Description

    Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride (LDK378 dihydrochloride) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride (LDK378 dihydrochloride) shows great antitumor potency[1][2].

    IC50 & Target

    IC50: 0.2 nM (ALK), 8 nM (IGF-1R), 7 nM (InsR), 23 nM (STK22D)[1]

    In Vitro

    Ceritinib (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].

    In Vivo

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

    Clinical Trial
    Molecular Weight

    631.06

    Formula

    C₂₈H₃₈Cl₃N₅O₃S

    CAS No.

    1380575-43-8

    SMILES

    CC(C)OC1=CC(C2CCNCC2)=C(C)C=C1NC3=NC=C(Cl)C(NC4=CC=CC=C4S(=O)(C(C)C)=O)=N3.[H]Cl.[H]Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    H2O : ≥ 170 mg/mL (269.39 mM)

    DMSO : 100 mg/mL (158.46 mM; Need ultrasonic)

    * "≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5846 mL 7.9232 mL 15.8464 mL
    5 mM 0.3169 mL 1.5846 mL 3.1693 mL
    10 mM 0.1585 mL 0.7923 mL 1.5846 mL
    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。 -80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 2.5 mg/mL (3.96 mM); Clear solution; Need ultrasonic

      此方案可获得 2.5 mg/mL (3.96 mM)的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,澄清透明的生理盐水溶液
    • 2.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (3.96 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (3.96 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定溶至 10 mL,完全溶解,澄清透明
    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (3.96 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (3.96 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 MCE 网站选购。
    References
    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    CeritinibLDK378LDK 378LDK-378ALKInsulin ReceptorIGF-1RAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Insulin-like growth factor-1 receptorInhibitorinhibitorinhibit

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    产品名称:
    Ceritinib dihydrochloride
    目录号:
    HY-15656A
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