2. Protein Tyrosine Kinase/RTK Stem Cell/Wnt JAK/STAT Signaling Epigenetics
  3. JAK Itk
  4. Modzatinib

Modzatinib (ITK kinase-IN-1) is an oral active, selective, covalent ITK/JAK3 dual-target inhibitor with IC50 values of 8 nM and 23 nM, respectively. Modzatinib exhibits anti-inflammatory activity and can be used in the research of autoimmune and inflammatory diseases.

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Modzatinib

Modzatinib Chemical Structure

CAS No. : 2411407-25-3

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Modzatinib Related Antibodies

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JAK1 JAK2 JAK3 Tyk2 JAK

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Description

Modzatinib (ITK kinase-IN-1) is an oral active, selective, covalent ITK/JAK3 dual-target inhibitor with IC50 values of 8 nM and 23 nM, respectively. Modzatinib exhibits anti-inflammatory activity and can be used in the research of autoimmune and inflammatory diseases[1].

IC50 & Target

JAK3

 

In Vitro

Modzatinib (Compound I) (0.01-1000 ng/mL; 2-18 h) inhibits aCD3/CD28-induced IL2/IFNγ mRNA and IL15-induced pSTAT5 in whole blood[1].

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

Modzatinib Related Antibodies
In Vivo

Modzatinib (5-15 mg/kg; oral gavage; BID; 14 days) dose-dependently reduces ankle swelling in a rat AIA model[1].
Modzatinib (100-300 ppm; diet admixed; QD; 35 days) dose-dependently ameliorates inflammatory injury in the colon and ileum in a mouse T-cell transfer colitis model[1].

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

Animal Model: C57BL/6 mice (male, ~20 g, 6-8 weeks); T cell transfer-induced inflammatory bowel disease[1]
Dosage: 100 ppm, 300 ppm
Administration: diet admixed, QD, 35 days
Result: Dose-dependently decreased histopathological scores in proximal colon, distal colon and ileum, and showed better protective effects than anti-IL12p40 antibody.
Molecular Weight

361.39

Formula

C18H21F2N5O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(F)(C1)[C@H]1C2=CNC3=NC=NC(N[C@H]4CN([C@H](CC4)C)C(C=C)=O)=C23
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 6.25 mg/mL (17.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7671 mL 13.8355 mL 27.6709 mL
5 mM 0.5534 mL 2.7671 mL 5.5342 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7671 mL 13.8355 mL 27.6709 mL 69.1773 mL
5 mM 0.5534 mL 2.7671 mL 5.5342 mL 13.8355 mL
10 mM 0.2767 mL 1.3835 mL 2.7671 mL 6.9177 mL
15 mM 0.1845 mL 0.9224 mL 1.8447 mL 4.6118 mL
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Modzatinib Related Classifications

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:

Modzatinib2411407-25-3ITK kinase-IN-1JAKItkJanus kinaseInterleukin-2 inducible T-cell kinaseIL2 inducible T-cell kinaseITK/JAK3Inhibitorinhibitorinhibit

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