CZC24832

For research use only.

Catalog No.S7018

8 publications

CZC24832 Chemical Structure

Molecular Weight(MW): 364.4

CZC24832 is the first selective PI3Kγ inhibitor with IC50 of 27 nM, with 10-fold selectivity over PI3Kβ and >100-fold selectivity over PI3Kα and PI3Kδ.

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Selleck's CZC24832 has been cited by 8 publications

3 Customer Reviews

  • (c) MM primary cells were treated with idelalisib (1 μm), CZC24832 (1 μm) and duvelisib (1 μm) for 72 h and then assessed for apoptosis by PI/Annexin V staining (n=4).

    Blood Cancer J, 2017, 7(3):e539. CZC24832 purchased from Selleck.

    For protein analysis, polymorphonuclear neutrophils (PMN) were activated with indicated stimuli (anti-TREM-1 antibody, matched control mAb, LPS) for 30 min after preincubated with idelalisib. Proteins were extracted with an urea-based lysis buffer, SDS PAGE was performed and proteins were blotted by a semi-dry process. Protein activation was analyzed by staining of phosphorylated and non-phosphorylated proteins. ß-actin served as loading control.

    Sci Rep, 2018, 8(1):5558. CZC24832 purchased from Selleck.

  • Effect of PI3Kγ inhibitor on Akt phosphorylation. JVM3 cells were pre-incubated with the indicated concentrations of CZC4832 (in μM) and then stimulated with SDF1α for 10 min. Akt Ser473 phosphorylation and total Akt levels were assessed by Western blot.

    Leukemia, 2018, 32(9):1958-1969. CZC24832 purchased from Selleck.

Purity & Quality Control

Choose Selective PI3K Inhibitors

Biological Activity

Description CZC24832 is the first selective PI3Kγ inhibitor with IC50 of 27 nM, with 10-fold selectivity over PI3Kβ and >100-fold selectivity over PI3Kα and PI3Kδ.
Targets
PI3Kγ [1]
(Cell-free assay)
PI3Kβ [1]
(Cell-free assay)
27 nM 1.1 μM
In vitro

CZC24832 has excellent selectivity to PI3Kγ. Out of the 154 identified lipid and protein kinases and the 922 other proteins, only two off targets (PI3Kβ and PIP4K2C) are detected within a 100-fold selectivity window. Despite the high sequence conservation of the human and rodent class I PI3K isoforms, the potency of CZC24832 for PI3Kγ and PI3Kβ is consistently lower by a factor of 2 to 4 in mice and rats compared to humans, but selectivity windows are largely retained. In the BT system, treatment with CZC24832 results in profound inhibition of IL-17A (IC50 =1.5 μM) as well as of B-cell activation markers such as IL-6 and IgG. In addition, strong inhibition of IL17A production is observed in T-cell systems such as human umbilical vein endothelial cells grown in the presence of TH2 blasts, indicating a general role for PI3Kγ kinase activity in the control of TH17 function. Thus, CZC24832 inhibits TH17 cell differentiation. [1]

In vivo In an IL-8–dependent air pouch model, CZC24832 shows a dose dependent reduction of granulocyte recruitment consistent with the degree of inhibition observed in PI3Kγ-null mice. In a therapeutic collagen induced arthritis (CIA) model, mice treated orally with 10 mg CZC24832 per kg body weight twice per day shows a substantial decrease of bone and cartilage destruction as well as of overall clinical parameters. [1]

Protocol

Animal Research:[1]
- Collapse
  • Animal Models: therapeutic mouse CIA model
  • Dosages: 3 mg/kg, 10 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 5 mg/mL warmed (13.72 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% CMC
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 364.4
Formula

C15H17FN6O2S

CAS No. 1159824-67-5
Storage powder
in solvent
Synonyms N/A
Smiles CC(C)(C)N[S](=O)(=O)C1=CN=CC(=C1)C2=C[N]3N=C(N)N=C3C(=C2)F

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID