1. PI3K/Akt/mTOR
  2. PI3K
  3. CZC24832

CZC24832 

Cat. No.: HY-15294 Purity: 99.46%
Handling Instructions

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

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

CZC24832 Chemical Structure

CZC24832 Chemical Structure

CAS No. : 1159824-67-5

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 125 In-stock
Estimated Time of Arrival: December 31
5 mg USD 114 In-stock
Estimated Time of Arrival: December 31
10 mg USD 166 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target

PI3Kγ

27 nM (IC50)

PI3Kβ

1.1 μM (IC50)

PI3Kδ

8.194 μM (IC50)

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].

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].

Molecular Weight

364.40

Formula

C₁₅H₁₇FN₆O₂S

CAS No.

1159824-67-5

SMILES

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

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 : ≥ 53 mg/mL (145.44 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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].

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.

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

References
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Keywords:

CZC24832CZC 24832CZC-24832PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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Product name:
CZC24832
Cat. No.:
HY-15294
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