2. Protein Tyrosine Kinase/RTK
  3. Itk
  4. GNE-9822

GNE-9822 is a potent, orally active and selective ITK inhibitor with a Ki value of 0.7 nM, and an EC50 value of 354.5 nM. GNE-9822 has good ADME properties. GNE-9822 can be used in research of asthma.

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

GNE-9822 Chemical Structure

GNE-9822 Chemical Structure

CAS No. : 1557232-32-2

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10 mg USD 880 In-stock
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Based on 1 publication(s) in Google Scholar

GNE-9822 Related Antibodies

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Description

GNE-9822 is a potent, orally active and selective ITK inhibitor with a Ki value of 0.7 nM, and an EC50 value of 354.5 nM. GNE-9822 has good ADME properties. GNE-9822 can be used in research of asthma[1][2].

IC50 & Target

EC50: 354.5 nM (ITK)[2]
In Vitro

GNE-9822 (compound 28) inhibits the phosphorylation of PLCγ with an IC50 value of 55 nM[1].

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

GNE-9822 Related Antibodies
In Vivo

GNE-9822 (compound 28; po and iv; 1 and 5 mg/kg) has good bioavailability and halflives observed in mouse and rats[1].

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

Animal Model: BALB/c mouse and Sprague-Dawley rats[1]
Dosage: 1 and 5 mg/kg
Administration: po (5 mg/kg) and iv (1 mg/kg)
Result: 1.19
species route dose volume (mL/kg) dose (mg/kg) Cmax (μM) AUC (μM·h) Cl (mL/min/kg) T1/2 (h) Vss (L/kg) %F
mouse (BALB/c) IV 1.0 1.0 1.5 40 2.9 10
mouse (BALB/c) PO 5.0 50 3.8 2.7 36
Animal Model: BALB/c mouse and Sprague-Dawley rats[1]
Dosage: 1 and 5 mg/kg
Administration: po (5 mg/kg) and iv (1 mg/kg)
Result: 1.19
species route dose volume (mL/kg) dose (mg/kg) Cmax (μM) AUC (μM·h) Cl (mL/min/kg) T1/2 (h) Vss (L/kg) %F
rat (Sprague-Dawley IV 1.0 1.0 0.6 70 3.0 14
rat (Sprague-Dawley PO 2.0 5.0 0.2 1.1 40
Molecular Weight

420.55

Formula

C24H32N6O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CN(C)CC[C@H](N1N=CC(NC(C2=NNC3=C2CCC(C)(C)C3)=O)=C1)C4=CC=CC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (148.61 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 2.3778 mL 11.8892 mL 23.7784 mL
5 mM 0.4756 mL 2.3778 mL 4.7557 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.

  • Molarity Calculator

  • Dilution Calculator

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 2.3778 mL 11.8892 mL 23.7784 mL 59.4460 mL
5 mM 0.4756 mL 2.3778 mL 4.7557 mL 11.8892 mL
10 mM 0.2378 mL 1.1889 mL 2.3778 mL 5.9446 mL
15 mM 0.1585 mL 0.7926 mL 1.5852 mL 3.9631 mL
20 mM 0.1189 mL 0.5945 mL 1.1889 mL 2.9723 mL
25 mM 0.0951 mL 0.4756 mL 0.9511 mL 2.3778 mL
30 mM 0.0793 mL 0.3963 mL 0.7926 mL 1.9815 mL
40 mM 0.0594 mL 0.2972 mL 0.5945 mL 1.4861 mL
50 mM 0.0476 mL 0.2378 mL 0.4756 mL 1.1889 mL
60 mM 0.0396 mL 0.1982 mL 0.3963 mL 0.9908 mL
80 mM 0.0297 mL 0.1486 mL 0.2972 mL 0.7431 mL
100 mM 0.0238 mL 0.1189 mL 0.2378 mL 0.5945 mL
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GNE-9822 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:

GNE-98221557232-32-2GNE9822GNE 9822ItkInterleukin-2 inducible T-cell kinaseIL2 inducible T-cell kinasephosphorylationPLCγbioavailabilityhalflivesorally activeInhibitorinhibitorinhibit

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