| Identification | Back Directory | [Name]
CZC24832 | [CAS]
1159824-67-5 | [Synonyms]
CS-957
CZC24832
CZC24832 USP/EP/BP
CZC 24832;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)-3-pyridinesulfonamide
5-(2-Amino-8-fluoro[1,2,4]triazolo[1,5-a]pyridin-6-yl)-N-(1,1-dimethylethyl)-3-pyridinesulfonamide
3-Pyridinesulfonamide, 5-(2-amino-8-fluoro[1,2,4]triazolo[1,5-a]pyridin-6-yl)-N-(1,1-dimethylethyl)-
CZC 24832
5-(2-Amino-8-fluoro[1,2,4]triazolo[1,5-a]pyridin-6-yl)-N-(tert-butyl)-3-pyridinesulfonamide
5-(2-Amino-8-fluoro[1,2,4]triazolo[1,5-a]pyridin-6-yl)-N-(tert-butyl)-3-pyridinesulfonamide CZC 24832 | [EINECS(EC#)]
200-258-5 | [Molecular Formula]
C15H17FN6O2S | [MDL Number]
MFCD22417090 | [MOL File]
1159824-67-5.mol | [Molecular Weight]
364.4 |
| Chemical Properties | Back Directory | [density ]
1.51 | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; insoluble in EtOH; ≥6.07 mg/mL in DMSO with gentle warming | [form ]
solid | [pka]
10.29±0.50(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
CZC24832 is a selective phosphoinositide 3-kinase γ (PI3Kγ) inhibitor. CZC24832 regulates interleukin-17-producing T helper cell (TH17) differentiation by PI3Kγ thus making CZC24832 a potential treatment for inflammatory and autoimmune diseases. | [Biological Activity]
CZC24832 is a potent and selective inhibitor of phosphoinositide 3-kinase γ (PI3Kγ) with Kd app of 19 nM. CZC24832 is said to be the first selective PI3Kγ inhibitor with efficacy in in vitro and in vivo models of inflammation. CZC24832 strongly inhibited T-cell interleukin 17A (IL-17A) production by inhibiting expression of retinoic acid receptor–related orphan receptor γt (RORγt)a transcription factor th at drives TH17 differentiationshowing a new role for PI3Kγ. | [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]. | [IC 50]
PI3Kγ: 27 nM (IC50); PI3Kβ: 1.1 μM (IC50); PI3Kδ: 8.194 μM (IC50) |
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