1. Protein Tyrosine Kinase/RTK
    Neuronal Signaling
    Autophagy
  2. ROS
    Trk Receptor
    ALK
    Autophagy
  3. Entrectinib

Entrectinib (Synonyms: NMS-E628; RXDX-101)

製品番号: HY-12678 純度: 99.32%
取扱説明書

Entrectinib (NMS-E628) is a potent, orally available, and CNS-active pan-Trk, ROS1, and ALK inhibitor. Entrectinib inhibits TrkA, TrkB, TrkC, ROS1 and ALK with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Antitumor activity.

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Entrectinib 構造式

Entrectinib 構造式

CAS 番号 : 1108743-60-7

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1  mL in DMSO USD 74 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 60 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 90 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 190 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 330 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Entrectinib purchased from MCE. Usage Cited in: Mol Cancer Ther. 2017 Oct;16(10):2130-2143.

    KM12 or CR20 cells are treated with increasing concentrations of Cabozantinib, Entrectinib or LOXO-101 for 3 hours. Cell lysates are immunoblotted to detect the indicated proteins.
    • 生物活性

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    • 参考文献

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    製品説明

    Entrectinib (NMS-E628) is a potent, orally available, and CNS-active pan-Trk, ROS1, and ALK inhibitor. Entrectinib inhibits TrkA, TrkB, TrkC, ROS1 and ALK with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Antitumor activity.

    IC50 & Target

    IC50: 1 nM (TrkA), 1 nM (TrkB), 1 nM (TrkC), 1 nM (ROS1),1 nM (ALK)[1]

    体外実験

    Entrectinib (NMS-E628) is found to be exquisitely active in inhibiting the proliferation of a limited number of cell lines: the TRKA-driven colorectal carcinoma cell line KM12 (IC50 of 17 nM), the ALK-dependent ALCL cell lines SU-DHL-1, Karpas-299, SUP-M2 and SR-786 (IC50 of 20, 31, 41, and 81 nM, respectively), the ALK-dependent NSCLC cell line NCI-H2228 (IC50 of 68 nM) and the FLT3-dependent AML cell line MV-4-11 (IC50 of 81 nM). Entrectinib potently blocks proliferation of Ba/F3-TEL-TRKB (IC50 of 2.9 nM), Ba/F3-TEL-TRKC (IC50 of 3.3 nM), and Ba/F3-TEL-ROS1 (IC50 of 5.3 nM) cells, with a high degree of selectivity versus parental Ba/F3 cells or those transformed by nontargeted kinases such as ABL and RET, which are inhibited with IC50s in the range of 2 to 3 μM[1]. Entrectinib significantly inhibits the growth of TrkB-expressing NB cells in vitro, and it significantly enhances the growth inhibition of Irino-TMZ when used in combination[2].

    体内実験

    Oral administration of entrectinib to tumor-bearing mice induces regression in relevant human xenograft tumors, including the TRKA-dependent colorectal carcinoma KM12, ROS1-driven tumors, and several ALK-dependent models of different tissue origins, including a model of brain-localized lung cancer metastasis[1]. Single agent therapy results in significant tumor growth inhibition in animals treated with entrectinib compared to control animals[2].

    臨床実験
    分子量

    560.64

    分子式

    C₃₁H₃₄F₂N₆O₂

    CAS 番号

    1108743-60-7

    SMILES

    O=C(NC1=NNC2=C1C=C(CC3=CC(F)=CC(F)=C3)C=C2)C4=C(NC5CCOCC5)C=C(N6CCN(C)CC6)C=C4

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 31 mg/mL (55.29 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7837 mL 8.9184 mL 17.8368 mL
    5 mM 0.3567 mL 1.7837 mL 3.5674 mL
    10 mM 0.1784 mL 0.8918 mL 1.7837 mL
    *Please refer to the solubility information to select the appropriate solvent.
    体内:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.46 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.46 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    参考文献
    細胞実験
    [2]

    NLF, NLF-TrkB, SY5Y or SY5Y-TrkB cells are plated in 96 well plates, and they are exposed to drug at different concentrations (1, 5, 10, 20, 30, 50 and 100 nM of entrectinib, 1.5 μM Irino and 50 μM TMZ, respectively) for one hr followed by addition of 100 ng/mL of BDNF. Plates are harvested at 24, 48, and 72 hr following addition of drug. The plates are processed and cell viability is analyzed using a standard SRB assay protocol[2].

    MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [2]

    Mice: Entrectinib is reconstituted in 0.5% methylcellulose containing 1% Tween 80 at a final dosing volume of 10 mL/kg (e.g., 0.2 mL for a 20 gm mouse). Treatment with entrectinib, Irino and TMZ started about 15–17 days after tumor inoculation when the average tumor size is 0.2 cm3. Mice are sacrificed when tumor volume reached 3 cm3. Tumors are harvested and flash frozen on dry ice for analysis of protein expression[2].

    MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献

    純度: 99.32%

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    Keywords:

    EntrectinibNMS-E628RXDX-101RXDX101RXDX 101ROSTrk ReceptorALKAutophagyTropomyosin related kinase receptor Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Inhibitorinhibitorinhibit

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    製品名:
    Entrectinib
    製品番号:
    HY-12678
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