2. Protein Tyrosine Kinase/RTK
  3. Anaplastic lymphoma kinase (ALK) Insulin Receptor IGF-1R
  4. Ceritinib mesylate

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

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CAS No. : 2055376-74-2

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Ceritinib mesylate 的其他形式现货产品:

Customer Review

Other Forms of Ceritinib mesylate:

Ceritinib mesylate 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 39 篇科研文献

Cell Proliferation/Viability Assay
Cell Imaging/Staining
WB
In Vivo Efficacy Study

    Ceritinib mesylate purchased from MCE. Usage Cited in: Nat Commun. 2024 Apr 23;15(1):3422.  [Abstract]

    At 48 h following transfection, the cells were treated with increasing concentrations of ceritinib for 72 h.

    Ceritinib mesylate purchased from MCE. Usage Cited in: Nat Cancer. 2022 Oct;3(10):1211-1227.  [Abstract]

    Oral olaparib (50 mg/kg) and ceritinib (7.5 mg/kg), either alone or in combination, five times per week, Tumor volume and Kaplan–Meier survival curves of mice bearing subcutaneous injected SKOV3 ovarian tumors.

    Ceritinib mesylate purchased from MCE. Usage Cited in: Nat Cancer. 2022 Oct;3(10):1211-1227.  [Abstract]

    Western blot analysis of indicated proteins in PARPi-sensitive triple-negative breast cancer (TNBC) cells (parental) and TNBC cells with acquired resistance to PARPi (#6 and #15) treated with 50 nM PARPi (talazoparib) or 0.5 µM ALK inhibitor (ALKi; ceritinib), either alone or in combination, for 48 hours.

    Ceritinib mesylate purchased from MCE. Usage Cited in: Nat Cancer. 2022 Oct;3(10):1211-1227.  [Abstract]

    Representative images of clonogenic assay results in PARPiresistant ovarian and TNBC cells in the presence of the indicated inhibitor for 12 days. Synergistic inhibition of cell proliferation is defined as CI < 1. CER, ceritinib; OLA, olaparib; Comb, combination of ceritinib and olaparib.

    Ceritinib mesylate purchased from MCE. Usage Cited in: Cell Discov. 2021 May 11;7(1):33.  [Abstract]

    BEAS-2B cells were transfected with GFP–EML4–ALK for 24 h. Cells were treated with DMSO or ALK inhibitors, alectinib (500 nM), ceritinib (500 nM), and GFP fluorescence was monitored through live imaging for up to 12 h.

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

    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

    生物活性

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

    体外研究
    (In Vitro)

    Ceritinib (LDK378) 还抑制 RET (IC50=400 nM)、FGFR3 (IC50=430 nM)、LCK (IC50= 560 nM)，JAK2 (IC50=610 nM)，Aurora (IC50=660 nM)，LYN (50=840 nM)，EGFR (IC50=900 nM)，FGFR4 (IC50=950 nM)[1]。
    Ceritinib (LDK378) 对 ALK 酶活性保持高效力，IC50 值为 200 pM，并且仅对一组 46 种激酶中的 IGF-1R、InsR 和 STK22D 具有强抑制作用，具有最低选择性为 70 倍。在转染各种激酶的 Ba/F3 细胞中，Ceritinib 抑制 ALK 活性，IC50 值为 40.7 nM，IC50 值 >100 nM 对抗所有其他测试的激酶. Ceritinib (LDK378) 在携带 NPM-ALK 融合基因的 Karpas 299 人非霍奇金 Ki 阳性大细胞淋巴瘤中显示出有效的抗增殖活性，IC50 值为 22.8 nM基因和 26 nM 在转染了 NPM-ALK 融合基因的 Ba/F3 细胞中。Ceritinib 对野生型 Ba/F3 细胞 (IC50>2 μM) 和转染 Tel-InsR 基因的 Ba/F3 细胞 (IC50=320) 也表现出良好的选择性nM)[2]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Ceritinib mesylate 相关抗体:
    体内研究
    (In Vivo)

    Ceritinib (LDK378) has an excellent pharmacokinetics profile in rodents and non-rodents with an oral bioavailability of >50%. Ceritinib demonstrates dose-dependent tumor growth inhibition and achieved partial tumor regression in the Karpas 299 rat xenograft model with daily administration but is capable of achieving complete tumor regression in the H2228 NSCLC rat xenograft model, which carries the EML4-ALK fusion gene. In both models, Ceritinib (LDK378) is well tolerated in animals. Ceritinib (LDK378) is further assessed for its ADME profile and is found to have a relatively good metabolic stability in liver microsomes, modest CYP3A4 inhibition, some hERG inhibition with an IC50 value of 46 μM in hERG patch clamp experiments, but no evidence of QTc prolongation in both dog and monkey telemetry studies[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    750.35

    Formula

    C30H44ClN5O9S3
    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献

    Ceritinib mesylate 相关分类

    • 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)

    质量   浓度   体积   分子量 *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Ceritinib2055376-74-2LDK378LDK 378LDK-378Anaplastic lymphoma kinase (ALK)Insulin ReceptorIGF-1RAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Insulin-like growth factor-1 receptorInhibitorinhibitorinhibit

    您最近查看的产品:

    Your information is safe with us. * Required Fields.

       产品名称：

    		  

    * 需求量：

    * 客户姓名：

    		 

    * Email：

    * 电话：

    		 

    * 公司或机构名称：

       留言给我们：

    Bulk Inquiry

    Inquiry Information

    产品名称：
    Ceritinib mesylate
    目录号：
    HY-15656B
    需求量：

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

       产品名称：

    		  

    * Lot #：

    * 客户姓名：

    		 

    * Email：

       电话：

    		 

    * 部门：

    * 公司或机构名称：

    		 

       留言给我们：

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.

    嗨！很高兴为您提供帮助！

    尊敬的 MCE 客户您好，
    请您选择所在区域，我们将转接对应客服为您服务！

    热门区域

    A

    B

    C

    F

    G

    H

    J

    L

    N

    Q

    S

    T

    X

    Y

    Z

    热 A B C F G H J L N Q S T X Y Z