ALK/ROS1-IN-1

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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

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]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	3.64 μM Compound: 2e	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31260890]
BaF3	IC₅₀	104.7 nM Compound: 2e	Antiproliferative activity against mouse BAF3 cells expressing CD74/ROS1 G2032R mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BAF3 cells expressing CD74/ROS1 G2032R mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 31260890]
BaF3	IC₅₀	137.7 nM Compound: 2e	Antiproliferative activity against mouse BAF3 cells expressing wild type CD74/ROS1 assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BAF3 cells expressing wild type CD74/ROS1 assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 31260890]
BaF3	IC₅₀	233.9 nM Compound: 2e	Antiproliferative activity against mouse BAF3 cells expressing CD74/ROS1 L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BAF3 cells expressing CD74/ROS1 L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 31260890]
HCC78	IC₅₀	10.71 μM Compound: 2e	Antiproliferative activity against ROS1-addicted human HCC78 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against ROS1-addicted human HCC78 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31260890]
NCI-H3122	IC₅₀	6.45 μM Compound: 2e	Antiproliferative activity against ALK-addicted human NCI-H3122 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against ALK-addicted human NCI-H3122 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31260890]

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 ALK^L1196M 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].

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

Molecular Weight

584.63

Formula

C₃₀H₃₅F₃N₆O₃

CAS No.

2365497-07-8

SMILES

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

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

Handling Instructions (2659 KB)

References

[1]. Liu S, et al. Design, synthesis and biological evaluations of 2-amino-4-(1-piperidine) pyridine derivatives as novel anti crizotinib-resistant ALK/ROS1 dual inhibitors. Eur J Med Chem. 2019 Oct 1;179:358-375. [Content Brief]

ALK/ROS1-IN-1 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-12365497-07-8Anaplastic lymphoma kinase (ALK)ROS KinaseAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246crizotinib-resistantALK/ROS1non-small-celllungcancerInhibitorinhibitorinhibit

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