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Cat. No.: HY-184275

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ITK-IN-7

ITK-IN-7 is a selective ITK inhibitor with an IC₅₀ of 16 nM and a K_i of 0.48 nM. ITK-IN-7 reduces IL-2 secretion levels in T cells and in mouse models stimulated by anti-CD3 monoclonal antibodies. ITK-IN-7 can be used for basic and translational research related to ITK inhibition, such as research on leukemia.

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

CAS No.: 3126105-55-0
Formula: C₂₇H₃₅N₇O₂
Molecular Weight:489.61

Storage:

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

ITK-IN-7 Chemical Structure

CAS No.: 3126105-55-0

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Use of MCE Products

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

Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

All ERK Isoforms :

In Vitro

OthersCytokines and ChemokinesAnti-cancer

Others

ITK-IN-7 (compound 19) (1 μM) potently inhibits ITK and exhibits exceptional selectivity over 24 other tested kinases, including BTK and key TCR pathway kinases^[1].

Others

ITK-IN-7 inhibits recombinant BTK kinase activity with an IC₅₀ of 5059 nM, representing over 300-fold selectivity for ITK over BTK^[1].

Others

ITK-IN-7 (0.01-10 μM; 4 h) potently inhibits PLCγ1 phosphorylation in Jurkat cells with an EC₅₀ of 15 nM and dose-dependently inhibits ERK phosphorylation^[1].

Others

ITK-IN-7 (3 μM; 4 h) induces sustained inhibition of PLCγ1 phosphorylation in Jurkat cells for over 12 h post-washout^[1].

Cytokines and Chemokines

ITK-IN-7 (range of concentrations; 4 h pretreatment, 24 h stimulation) potently inhibits IL-2 secretion in TCR-stimulated Jurkat cells with an EC₅₀ of 19 nM^[1].

Anti-cancer

ITK-IN-7 (range of concentrations; 72 h) inhibits proliferation of Jurkat, MOLT-4, and CCRF-CEM T-cell leukemia cells with GI₅₀ values of 0.8 μM, 3.4 μM, and 2.6 μM, respectively, and exhibits reduced activity against B-cell lines and non-malignant HEK293T cells^[1].

Others

ITK-IN-7 (0.03-10 μM) does not inhibit BTK-mediated PLCγ2 phosphorylation in Namalwa B cells, confirming excellent cellular selectivity for ITK over BTK^[1].

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

Parmacokinetics

Species	Dose	Route	C₀	T_1/2	AUC_0-t	AUC_0-∞	V_z	CL	V_ss	MRT
Mice^[1]	2 mg/kg	i.p.	3473 ng/mL	2.19 h	555 ng·h/mL	561 ng·h/mL	11.6 L/kg	62.7 mL/min/kg	2.51 L/kg	0.53 h

In Vivo

Adaptive ImmunityCytokines & Chemokines

Adaptive Immunity

Cytokines & Chemokines

ITK-IN-7 (compound 19) (50-100 mg/kg; i.p.; single dose) potently and sustainably inhibits anti-CD3 mAb-induced IL-2 production in female BALB/c mice^[1].

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

Animal Model:

BALB/c (female)^[1]
Dosage:

50 mg/kg; 100 mg/kg
Administration:

i.p.; single dose
Result:

Reduced serum IL-2 levels by nearly 50% compared to the vehicle group when measured 3 hours post-dose at 50 mg/kg.
Reduced serum IL-2 levels by approximately 80% compared to the vehicle group when measured 3 hours post-dose at 100 mg/kg.
Maintained over 70% IL-2 suppression when measured 8 hours post-dose at 100 mg/kg.

Chemical Information

CAS No. 3126105-55-0
Molecular Weight 489.61
Formula C₂₇H₃₅N₇O₂
SMILES

O=C(C1=NNC2=C1CCC(C)(C)C2)NC3=CN([C@H](C4=CC=CC=C4)CCN(C)C)N=C3NC(C=C)=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]. Ruan Z, et al.. Discovery of pyrazole-based selective covalent ITK inhibitors with In vivo activity. European journal of medicinal chemistry. 2026 May 30;316:119025. [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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Biological Activity
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- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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ITK-IN-7

All ERK Isoforms

Biological Activity

Description

In Vitro

Parmacokinetics

In Vivo

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

ITK-IN-7 Related Classifications

HY-184275 Related Classifications

Bioz

Keywords

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