Home PI3K/Akt/mTOR PI3K inhibitor CZC24832 For research use only.

CZC24832

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.

CZC24832 Chemical Structure

CZC24832 Chemical Structure

CAS: 1159824-67-5

Selleck's CZC24832 has been cited by 14 Publications

3 Customer Reviews

Purity & Quality Control

Batch: S701801 DMSO] 5 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.88%
99.88

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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
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 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]
Animal Research Animal Models therapeutic mouse CIA model
Dosages 3 mg/kg, 10 mg/kg
Administration Orally

Chemical Information & Solubility

Molecular Weight 364.4 Formula

C15H17FN6O2S
CAS No. 1159824-67-5 SDF Download CZC24832 SDF
Smiles CC(C)(C)NS(=O)(=O)C1=CN=CC(=C1)C2=CN3C(=NC(=N3)N)C(=C2)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 5 mg/mL ( (13.72 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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

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