GNE-9822

Name: GNE-9822
Brand: MedChemExpress
SKU: HY-12410
Rating: 4.5 (1 reviews)

Cat. No.: HY-12410 Purity: ≥95.0%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

GNE-9822 is a potent, orally active and selective ITK inhibitor with a K_i 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

CAS No. : 1557232-32-2

Size	Price	Stock	Quantity
5 mg	USD 540	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 880	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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References
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Description

IC₅₀ & Target

EC50: 354.5 nM (ITK)^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
Jurkat	IC₅₀	0.045 μM Compound: 1, GNE-9822	Inhibition of ITK in TCR stimulated human Jurkat T cells assessed as reduction of PLC-gamma phosphorylation preincubated for 30 mins followed by TCR induction for 2 mins Inhibition of ITK in TCR stimulated human Jurkat T cells assessed as reduction of PLC-gamma phosphorylation preincubated for 30 mins followed by TCR induction for 2 mins	[PMID: 25844760]
Jurkat	IC₅₀	4.7 μM Compound: 1, GNE-9822	Cytotoxicity against human Jurkat T cells without TCR stimulation assessed as cell viability by ATPlite assay Cytotoxicity against human Jurkat T cells without TCR stimulation assessed as cell viability by ATPlite assay	[PMID: 25844760]
Jurkat	IC₅₀	55 nM Compound: 28	Inhibition of ITK in human Jurkat cells assessed as reduction in PLC-gamma phosphorylation after 30 mins Inhibition of ITK in human Jurkat cells assessed as reduction in PLC-gamma phosphorylation after 30 mins	[PMID: 24918870]

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.

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)	C_max (μM)	AUC (μM·h)	Cl (mL/min/kg)	T_1/2 (h)	V_ss (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)	C_max (μM)	AUC (μM·h)	Cl (mL/min/kg)	T_1/2 (h)	V_ss (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.

1557232-32-2

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
10 mM	0.2378 mL	1.1889 mL	2.3778 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: ≥95.0%

Select Batch:

Data Sheet (279 KB) SDS (251 KB)

COA (252 KB) HNMR (270 KB) MS (184 KB)

Handling Instructions (2659 KB)

References

[1]. Zhou D, et al. Discovery of Potent and Highly Selective Interleukin-2-Inducible T-Cell Kinase Degraders with In Vivo Activity. J Med Chem. 2023 Apr 13;66(7):4979-4998. [Content Brief]

[2]. Burch JD, et, al. Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors. J Med Chem. 2014 Jul 10;57(13):5714-27. [Content Brief]

Complete Stock Solution Preparation Table

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

GNE-9822 Related Classifications

Inflammation/Immunology

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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GNE-9822

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Complete Stock Solution Preparation Table

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