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Cat. No.: HY-146672

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ITK inhibitor 6

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.

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

CAS No.: 2404604-06-2
Formula: C₂₈H₂₄F₂N₄O₂
Molecular Weight:486.51

Storage:

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

Data Sheet (271 KB)

ITK inhibitor 6 Chemical Structure

CAS No.: 2404604-06-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

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.

Chemical Information

CAS No. 2404604-06-2
Molecular Weight 486.51
Formula C₂₈H₂₄F₂N₄O₂
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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