ITK inhibitor 6

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ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC₅₀s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities.

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ITK inhibitor 6 Chemical Structure

CAS No. : 2404604-06-2

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Description

IC₅₀ & Target

IC₅₀: 4 nM (ITK); 133 nM (BTK), 320 nM (JAK3), 2360 nM (EGFR), 155 nM (LCK)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	GI₅₀	3.4 μM Compound: 43	Antiproliferative activity against human CCRF-CEM cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo luminescence based assay Antiproliferative activity against human CCRF-CEM cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo luminescence based assay	[PMID: 31830635]
H9	GI₅₀	5.4 μM Compound: 43	Antiproliferative activity against human H9 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo luminescence based assay Antiproliferative activity against human H9 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo luminescence based assay	[PMID: 31830635]
HEK-293T	GI₅₀	19 μM Compound: 43	Cytotoxicity against human HEK293T cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo luminescence based assay Cytotoxicity against human HEK293T cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo luminescence based assay	[PMID: 31830635]
Jurkat	EC₅₀	119 nM Compound: 43	Inhibition of ITK in anti-CD3/CD28 beads-stimulated human Jurkat cells assessed as reduction in Plcgamma1 phosphorylation incubated for 2 hrs followed by stimulation with anti-CD3/CD28 beads by Western blot analysis Inhibition of ITK in anti-CD3/CD28 beads-stimulated human Jurkat cells assessed as reduction in Plcgamma1 phosphorylation incubated for 2 hrs followed by stimulation with anti-CD3/CD28 beads by Western blot analysis	[PMID: 31830635]
Jurkat	GI₅₀	5.1 μM Compound: 43	Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo luminescence based assay Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo luminescence based assay	[PMID: 31830635]
MOLT-4	GI₅₀	3.7 μM Compound: 43	Antiproliferative activity against human MOLT4 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo luminescence based assay Antiproliferative activity against human MOLT4 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo luminescence based assay	[PMID: 31830635]

In Vitro

ITK inhibitor 6 (compound 43) shows antiproliferative activities with GI₅₀s of 5.1, 3.7, 3.4, 5.4, 19 µM for Jurkat, Molt-4, CCRF-CEM, H9, HEK 293 T cells, respectively^[1].
ITK inhibitor 6 docks into the ATP-binding site of ITK and BTK^[1].

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

Molecular Weight

486.51

Formula

C₂₈H₂₄F₂N₄O₂

CAS No.

2404604-06-2

SMILES

C=CC(NCCOC1=C2C=C(NC2=CC(CC3=CC=CC=C3)=C1)C4=NNC5=C4C=CC(C(F)F)=C5)=O

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]. Wang X, et al. Design, synthesis and structure-activity relationship of indolylindazoles as potent and selective covalent inhibitors of interleukin-2 inducible T-cell kinase (ITK). Eur J Med Chem. 2020 Feb 1;187:111918. [Content Brief]

ITK inhibitor 6 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:

ITK inhibitor 62404604-06-2ITK inhibitor6ITK inhibitor-6ItkInterleukin-2 inducible T-cell kinaseIL2 inducible T-cell kinaseICR miceHEK 293 TJurkat cellsPLCγ1ERK1/2phosphorylation， antiproliferativeInhibitorinhibitorinhibit

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