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) 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].

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ALK/ROS1-IN-5 Chemical Structure

ALK/ROS1-IN-5 Chemical Structure

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ALK/ROS1-IN-5 Related Antibodies

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Description

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].

In Vitro

ALK/ROS1-IN-5 (0-100 μM, 72 h) exhibits superior inhibitory activity against both H2228, H1975 and H460 cells[1].
ALK/ROS1-IN-5 (10 μM) exhibits notable inhibitory activity against members of the tyrosine kinase family, including EGFR, AKT1, FGFR1 and ERK1[1].
ALK/ROS1-IN-5 (10 μM) demonstrates significant kinase inhibitory activity against ALK and ROS1, with inhibition rates of 94.34% and 94.27 %, respectively[1].
ALK/ROS1-IN-5 (1-2 μM, 24 h) inhibts cell migration in H2228 cells dose-dependently[1].
ALK/ROS1-IN-5 (1-2 μM, 24 h) induces apoptosis and cell cycle arrest in H2228 cells dose-dependently[1].
ALK/ROS1-IN-5 (1-2 μM, 24 h) induces in H2228 cells dose-dependently[1].
ALK/ROS1-IN-5 (0.1- 0.5 μM, 24 h) reduced the phosphorylation of ALK and ERK in a dose-dependent manner[1].

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

ALK/ROS1-IN-5 Related Antibodies

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.
In Vivo

ALK/ROS1-IN-5 (60, 120 mg/kg, p.o., daily, 7 days) exhibits no significant toxicity in biochemical blood samples in mice [1] .
ALK/ROS1-IN-5 (10 mg/kg, p.o., daily, 35 days) demonstrates great antitumor effect[1] .
ALK/ROS1-IN-5 (5-25 mg/kg, p.o., daily, 14 days) has minimal impact on RET (reduction of the reticulocyte) [1] .
ALK/ROS1-IN-5 (25-50 mg/kg, p.o., daily, 21 days) exhibits a lower tumor volume growth rate than the positive control group[1] .
ALK/ROS1-IN-5 decreases Ki67, Bcl2, Caspase 3 and PCNA in a dose-dependent manner as the dosage[1] .

MedChemExpress (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 %.
Molecular Weight

554.59

Formula

C32H28F2N4O3
SMILES

FC1=CC(F)=CC(CC2=CC=C(NN=C3NC(C4=CC=C(C5=CC=C(OC)C=C5)C=C4N6CCOCC6)=O)C3=C2)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ALK/ROS1-IN-5 Related Classifications

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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:

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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