CZC24832
CZC24832 Basic information
- Product Name:
- CZC24832
- Synonyms:
-
- CZC24832
- 5-(2-Amino-8-fluoro[1,2,4]triazolo[1,5-a]pyridin-6-yl)-N-(tert-butyl)-3-pyridinesulfonamide
- 3-Pyridinesulfonamide, 5-(2-amino-8-fluoro[1,2,4]triazolo[1,5-a]pyridin-6-yl)-N-(1,1-dimethylethyl)-
- 5-(2-Amino-8-fluoro[1,2,4]triazolo[1,5-a]pyridin-6-yl)-N-(tert-butyl)-3-pyridinesulfonamide CZC 24832
- 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-butylpyridine-3-sulfonamide
- CZC 24832;CZC-24832
- CS-957
- CAS:
- 1159824-67-5
- MF:
- C15H17FN6O2S
- MW:
- 364.4
- EINECS:
- 200-258-5
- Product Categories:
-
- Akt
- mTOR
- PI3K
- Inhibitors
- PI3K/Akt/mTOR
- Mol File:
- 1159824-67-5.mol
CZC24832 Chemical Properties
- 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
CZC24832 Usage And Synthesis
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 differentiation, showing 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)
CZC24832Supplier
- Tel
- sales@boylechem.com
- Tel
- 18210857532; 18210857532
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- +86-21-20908456
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