1. Protein Tyrosine Kinase/RTK
  2. ALK
    ROS
  3. ALK/ROS1-IN-1

ALK/ROS1-IN-1 

Cat. No.: HY-130794
Handling Instructions

ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.

For research use only. We do not sell to patients.

ALK/ROS1-IN-1 Chemical Structure

ALK/ROS1-IN-1 Chemical Structure

CAS No. : 2365497-07-8

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Description

ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.

IC50 & Target

IC50: 0.174 μM (ALK), 0.530 μM (ROS1)[1]

In Vitro

ALK/ROS1-IN-1 displays potent anti-proliferative activity against ALK-addicted H3122 and ROS1-addicted HCC78 cell lines (IC50= 6.27 μM and 10.71 μM, respectively)[1].
ALK/ROS1-IN-1 shows impressive enzyme activity against clinically Crizotinib-resistant ALKL1196M with an IC50 value of 41.3 nM[1].
ALK/ROS1-IN-1 shows potent inhibitory activity in Ba/F3 cell line expressing ROS1 mutants, with IC50s of 137.7, 104.7 nM and 233.9 for wide-type, G2032R mutant and L2026M mutant, respectively[1].
ALK/ROS1-IN-1 has no significant effect on inducing apoptosis of HCC78 cell line[1].

Molecular Weight

584.63

Formula

C₃₀H₃₅F₃N₆O₃

CAS No.

2365497-07-8

SMILES

O=C([[email protected]]1CCCN(C2=CC(NC3=CC=C(N4CCNCC4)C=C3OC)=NC=C2)C1)NCC5=CC=C(OC(F)(F)F)C=C5

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

ALK/ROS1-IN-1ALKROSAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246crizotinib-resistantALK/ROS1non-small-celllungcancerInhibitorinhibitorinhibit

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ALK/ROS1-IN-1
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