DC Chemicals · Product datasheet

CZC24832 — Datasheet

CAT. NO. DC7734

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ParameterValue
Chemical Name5-(2-Amino-8-fluoro-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-N-tert-butylpyridine-3-sulfonamide
CAS No.1159824-67-5
SynonymsCZC24832;5-(2-amino-8-fluoro-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-N-tert-butylpyridine-3-sulfonamide;CHEMBL2064571;CS-0710;CZC-24832;FD5029;HY-15294;SureCN936070;5-(2-Amino-8-fluoro[1,2,4]triazolo[1,5-a]pyridin-6-yl)-N-(1,1-dimethylethyl)-3-pyridinesulfonamide;5-(2-Amino-8-fluoro[1,2,4]triazolo[1,5-a]pyridin-6-yl)-N-(tert-butyl)-3-pyridinesulfonamide;CZC 24832;5-{2-amino-8-fluoro-[1,2,4]triazolo[1,5-a]pyridin-6-yl}-N-tert-butylpyridine-3-sulfonamide;5-(2-amino-8-fluoro-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-N-(tert-butyl)pyridine-3-sulfonamide;GTPL6653;AOB4312;HMS3652D16;BCP08888;s7018;BDBM50389420;SB17239;NCGC00379179;SW219482-1;CZC24832, >=98% (HPLC)
FormulaC15H17FN6O2S
M.Wt364.3979
SMILESS(C1=C([H])N=C([H])C(C2C([H])=C(C3=NC(N([H])[H])=NN3C=2[H])F)=C1[H])(N([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])(=O)=O
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

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

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].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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