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Details

Stereochemistry ACHIRAL
Molecular Formula C15H17FN6O2S
Molecular Weight 364.398
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CZC-24832

SMILES

CC(C)(C)NS(=O)(=O)C1=CN=CC(=C1)C2=CN3N=C(N)N=C3C(F)=C2

InChI

InChIKey=RXRZPHQBTHQXSV-UHFFFAOYSA-N
InChI=1S/C15H17FN6O2S/c1-15(2,3)21-25(23,24)11-4-9(6-18-7-11)10-5-12(16)13-19-14(17)20-22(13)8-10/h4-8,21H,1-3H3,(H2,17,20)

HIDE SMILES / InChI
Molecular Formula C15H17FN6O2S
Molecular Weight 364.398
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

CZC24832 is a highly selective and potent phosphoinositide 3-kinase γ (PI3Kγ) inhibitor. It dempnstrated efficacy in in vitro and in vivo models of inflammation.

Originator

Approval Year

Unknown
139594
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8297
 19.0 nM [Kd]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Preclinical
Unknown

Approved Use

Unknown
PubMed

PubMed

TitleDatePubMed
A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation.
2012 Apr 29
SAR studies around a series of triazolopyridines as potent and selective PI3Kγ inhibitors.
2012 Aug 15
Patents

Patents

WO2016025656A1
3
WO2016190897A1
1
WO2016193955A1
1

Sample Use Guides

In Vivo Use Guide
10 mg/kg CZC24832 reduced the progression and severity of arthritis in a therapeutic mouse collagen-induced arthritis model.
Route of Administration: Oral
In Vitro Use Guide
CZC24832 was active in PI3Kγ-dependent cellular C5a-induced AKT Ser473 phosphorylation (IC50 = 1.2 μM) and fMLP-induced neutrophil migration assays (IC50 = 1.0 μM)
Substance Class Chemical
Created
by admin
on Sat Dec 16 18:08:18 UTC 2023
Edited
by admin
on Sat Dec 16 18:08:18 UTC 2023
Record UNII
96ER5DQD27
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
CZC-24832
Code English
5-(2-AMINO-8-FLUORO(1,2,4)TRIAZOLO(1,5-A)PYRIDIN-6-YL)-N-(1,1-DIMETHYLETHYL)-3-PYRIDINESULFONAMIDE
Systematic Name English
CZC24832
Code English
Code System Code Type Description
PUBCHEM
42623951
Created by admin on Sat Dec 16 18:08:18 UTC 2023 , Edited by admin on Sat Dec 16 18:08:18 UTC 2023
PRIMARY
CAS
1159824-67-5
Created by admin on Sat Dec 16 18:08:18 UTC 2023 , Edited by admin on Sat Dec 16 18:08:18 UTC 2023
PRIMARY
EPA CompTox
DTXSID50655226
Created by admin on Sat Dec 16 18:08:18 UTC 2023 , Edited by admin on Sat Dec 16 18:08:18 UTC 2023
PRIMARY
FDA UNII
96ER5DQD27
Created by admin on Sat Dec 16 18:08:18 UTC 2023 , Edited by admin on Sat Dec 16 18:08:18 UTC 2023
PRIMARY
Related Record Type Details
PHOSPHATIDYLINOSITOL 4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT GAMMA ISOFORM
TARGET -> INHIBITOR
Exhibited 10-fold selectivity over PI3Kβ and >100-fold selectivity over PI3Kα and PI3Kδ.
IC50
Related Record Type Details
Structure of CZC-24832
ACTIVE MOIETY
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