Referencia número: HY-15294

CZC24832

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

CZC24832 is a highly selective and potent PI3Kγ inhibitor (IC₅₀=27 nM) with apparent dissociation constants (K_d^app) of 19 nM.

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Pureza: 99.07%
No. CAS: 1159824-67-5
Fòrmula: C₁₅H₁₇FN₆O₂S
Peso molecular:364.40

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

CZC24832 Chemical Structure

No. CAS: 1159824-67-5

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

CZC24832 is a highly selective and potent PI3Kγ inhibitor (IC₅₀=27 nM) with apparent dissociation constants (K_d^app) of 19 nM.

IC₅₀ & Target^[1]

PI3Kγ

27 nM (IC₅₀)

PI3Kβ

1.1 μM (IC₅₀)

PI3Kδ

8.194 μM (IC₅₀)

Ver todos los productos específicos de isoformas PI3K :

In Vitro

CZC24832 is active in PI3Kγ-dependent cellular C5a-induced AKT Ser473 phosphorylation (IC₅₀=1.2 μM) and N-formyl-methionine-leucinephenylalanine (fMLP)-induced neutrophil migration assays (IC₅₀=1.0 μM)^[1].

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

In Vivo

CZC24832 shows suitable pharmacokinetic properties including low clearance (0.84 L per h per kg body weight) and high oral bioavailability (37%), thus allowing further characterization of the inhibitor in rodent models of inflammation. In an IL-8-dependent air pouch model, CZC24832 shows a dose-dependent reduction of granulocyte recruitment (80% inhibition at 10 mg per kg body weight) consistent with the degree of inhibition observed in PI3Kγ-null mice. Mice treated orally with 10 mg CZC24832 per kg body weight twice per day show a substantial decrease of bone and cartilage destruction (53% reduction by histopathological analysis) as well as of overall clinical parameters (38% reduction)^[1].

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

Chemical Information

No. CAS 1159824-67-5
Appearance Solid
Peso molecular 364.40
Fòrmula C₁₅H₁₇FN₆O₂S
Color White to off-white
SMILES

FC1=CC(C2=CC(S(=O)(NC(C)(C)C)=O)=CN=C2)=CN3C1=NC(N)=N3
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Int J Nanomedicine

PLGA-PEG Nano-Adjuvant-Delivered ClfA Vaccine Elicits IL-17A-Mediated Neutrophil Activation to Confer Complete Protection Against Methicillin-Resistant Staphylococcus aureus. [Abstract]

2026 Jun 3:21:592819. PMID: 42267312

Solvente y solubilidad

In Vitro:

DMSO : ≥ 53 mg/mL (145.44 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7442 mL

13.7212 mL

27.4424 mL

5 mM

0.5488 mL

2.7442 mL

5.4885 mL

10 mM

0.2744 mL

1.3721 mL

2.7442 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (6.86 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (6.86 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocolo

Cell Assay^[1]

RAW264.7 or THP-1 cells are starved for 2.5 h in serum-free medium before CZC24832 (0.1, 1, 10 and 100 μM) incubation for 30 min at 37°C. RAW264.7 cells are then stimulated for 3 min with C5a at a concentration of 0.6 μM, and THP-1 cells are stimulated with either insulin (1 uM, 10 min) or CSF (50 μg/mL, 5 min) at 37°C and lysed on ice. The detection of AKT phosphorylation (Ser473) is performed using the iBlot system^[1].

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

Animal Administration^[1]

Rats^[1]
Pharmacokinetics and oral bioavailability of CZC24832 are investigated in male Wistar rats following administration of a single intravenous (0.2 mg per kg body weight) or oral dose (10 mg per kg body weight). The dosing vehicle used is 0.5% (w/v) carboxymethyl cellulose in water for oral gavage. The intravenous dosing vehicle is 10% (v/v) DMSO in 30% (v/v) polyethylene glycol (PEG-400). Heparin blood for pharmacokinetic analysis is withdrawn retro-orbitally from mice or sublingually from rats to prepare plasma samples. These are homogenized with 10% (v/v) water and 3 volumes of acetonitrile and analyzed for CZC24832 by HPLC-MS/MS.

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Bergamini G, et al. A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation. Nat Chem Biol. 2012 Apr 29;8(6):576-82. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7442 mL	13.7212 mL	27.4424 mL	68.6059 mL
	5 mM	0.5488 mL	2.7442 mL	5.4885 mL	13.7212 mL
	10 mM	0.2744 mL	1.3721 mL	2.7442 mL	6.8606 mL
	15 mM	0.1829 mL	0.9147 mL	1.8295 mL	4.5737 mL
	20 mM	0.1372 mL	0.6861 mL	1.3721 mL	3.4303 mL
	25 mM	0.1098 mL	0.5488 mL	1.0977 mL	2.7442 mL
	30 mM	0.0915 mL	0.4574 mL	0.9147 mL	2.2869 mL
	40 mM	0.0686 mL	0.3430 mL	0.6861 mL	1.7151 mL
	50 mM	0.0549 mL	0.2744 mL	0.5488 mL	1.3721 mL
	60 mM	0.0457 mL	0.2287 mL	0.4574 mL	1.1434 mL
	80 mM	0.0343 mL	0.1715 mL	0.3430 mL	0.8576 mL
	100 mM	0.0274 mL	0.1372 mL	0.2744 mL	0.6861 mL

Keywords

CZC24832

1 Cited Publications

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CZC24832

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Publications Citing Use of MedChemExpress (MCE) CZC24832

Ver todos los productos específicos de isoformas PI3K

Actividad biológica

Chemical Information

Publications (1)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

CZC24832 Related Classifications

HY-15294 Related Classifications