2. Protein Tyrosine Kinase/RTK Apoptosis
  3. Anaplastic lymphoma kinase (ALK) ROS Kinase Apoptosis
  4. ALK/ROS1-IN-5

ALK/ROS1-IN-5 (compound X4) 是一种ALK 和 ROS1 激酶选择性抑制剂，IC50 分别为 0.512 (ALK)，0.766 μM (ROS1)。ALK/ROS1-IN-5 抑制 H2228 细胞，IC50 为 0.034 μM。ALK/ROS1-IN-5 以剂量依赖性方式诱导癌细胞 apoptosis。ALK/ROS1-IN-5 有效抑制癌细胞中 p-ALK 和 p-ERK 的表达。

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ALK/ROS1-IN-5 Chemical Structure

ALK/ROS1-IN-5 Chemical Structure

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ALK/ROS1-IN-5 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ALK/ROS1-IN-5 (compound X4) is a selective ALK and ROS1 kinases inhibitor with IC50s of 0.512 μM (ALK), 0.766 μM (ROS1), respectively. ALK/ROS1-IN-5 inhibits H2228 cells with an IC50 of 0.034 μM. ALK/ROS1-IN-5 induces cancer cells apoptosis in dose-dependent manner. ALK/ROS1-IN-5 effectively suppresses the expression of p-ALK and p-ERK in cancer cells[1].

体外研究
(In Vitro)

ALK/ROS1-IN-5 (0-100 μM, 72 h) 对 H2228，H1975 和 H460 细胞均具有优异的抑制活性[1]。
ALK/ROS1-IN-5 (10 μM) 对酪氨酸激酶家族成员，包括 EGFR，AKT1，FGFR1 和 ERK1 具有显著抑制活性[1]。
ALK/ROS1-IN-5 (10 μM) 对 ALK 和 ROS1 具有明显的激酶抑制活性，抑制率分别为 94.34% 和94.27%[1]。
ALK/ROS1-IN-5 (1-2 μM, 24 h) 剂量依赖性地抑制 H2228 细胞迁移[1]。
ALK/ROS1-IN-5 (1-2 μM, 24 h) 剂量依赖性地诱导 H2228 细胞凋亡和细胞周期阻滞[1]。
ALK/ROS1-IN-5 (0.1- 0.5 μM, 24 h) 以剂量依赖性方式降低 ALK 和 ERK 的磷酸化。[1]。

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

ALK/ROS1-IN-5 相关抗体:

Cell Cycle Analysis [1]

Cell Line: H2228 cells
Concentration: 1, 2 μM
Incubation Time: 24 h
Result: Significantly arrested the cell cycle of H2228 cells in the S phase, exhibiting a clear concentration-dependent effect.

Cell Migration Assay [1]

Cell Line: H2228 cells
Concentration: 1, 2 μM
Incubation Time: 24 h
Result: Dose-dependently and effectively inhibited wound healing in H2228 cells.

Cell Proliferation Assay [1]

Cell Line: H2228, H1975, H460 cells
Concentration: 0- 100 μM
Incubation Time: 72 h
Result: Inhibited H460 and H2228 cells with IC50 of 0.21 μM and 0.034 μM respectively.

Apoptosis Analysis [1]

Cell Line: H2228 cells
Concentration: 1, 2 μM
Incubation Time: 24 h
Result: Showed a 10.0 % late cell apoptosis rate compared to Entrectinib (HY-12678) at the same 2 μM dose of the positive drug.
Significantly promoted apoptosis in H2228 cells in a dose-dependent manner.

Western Blot Analysis [1]

Cell Line: H2228 cells
Concentration: 0.1, 0.2, 0.5 μM
Incubation Time: 24 h
Result: Reduced the phosphorylation of ALK and ERK in a dose dependent manner.
Not only effectively inhibited the expression of p-ALK in H2228 cells, but also inhibited the expression of p-ERK, a pathway downstream of ALK and ROS1 kinase.
体内研究
(In Vivo)

ALK/ROS1-IN-5 (60, 120 mg/kg, p.o., daily, 7 days) 对小鼠血液生化样品无明显毒性[1]。
ALK/ROS1-IN-5 (10 mg/kg, p.o., daily, 35 days) 显示出良好的抗肿瘤作用[1]。
ALK/ROS1-IN-5 (5-25 mg/kg, p.o., daily, 14 days) 对网织红细胞减少的影响最小[1]。
ALK/ROS1-IN-5 (25-50 mg/kg, p.o., daily, 21 days) 药物组的肿瘤体积生长率低于阳性对照组[1]。
ALK/ROS1-IN-5 以剂量依赖的方式降低 Ki67，Bcl2，Caspase 3 和 PCNA[1]。

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

Animal Model: KM mice [1] .
Dosage: 60, 120 mg/kg
Administration: p.o., daily, 7 days
Result: Exhibited no significant toxicity.
Animal Model: H2228 tumor-bearing nude mice [1] .
Dosage: 10 mg/kg
Administration: p.o., daily, 35 days
Result: In combination with weekly 37.5 mg/kg Carboplatin (HY-17393) demonstrated great improvement of the antitumor effect compared to carboplatin monotherapy (94.7% TGI vs 69.7% TGI).
Induced no significant body weight loss during the study.
Animal Model: H2228 tumor-bearing nude mice [1] .
Dosage: 5, 25 mg/kg
Administration: p.o., daily, 14 days
Result: Had minimal impact on RET (reduction of the reticulocyte).
Induced no significant body weight loss during the study.
Animal Model: H2228 tumor-bearing nude mice [1] .
Dosage: 25, 50 mg/kg
Administration: p.o., once every 48 h, 21days
Result: Exhibited a lower tumor volume growth rate than the positive control group.
Exhibited a tumor inhibition rate greater than 30 %.
分子量

554.59

Formula

C32H28F2N4O3
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

ALK/ROS1-IN-5 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

ALK/ROS1-IN-5Anaplastic lymphoma kinase (ALK)ROS KinaseApoptosisAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246non-small cell lung cancer (NSCLC)kinasesInhibitorinhibitorinhibit

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