- CZC24832
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- $1.00
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2020-01-13
- CAS:1159824-67-5
- Min. Order: 1g
- Purity: 99%
- Supply Ability: 1ton
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| | 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 | | 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) | | InChIKey | RXRZPHQBTHQXSV-UHFFFAOYSA-N | | SMILES | FC1=CC(C2=CN=CC(S(NC(C)(C)C)(=O)=O)=C2)=CN3C1=NC(N)=N3 |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids | | Hazard Classifications | Eye Irrit. 2
Skin Irrit. 2
STOT SE 3 |
| | 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) |
| | CZC24832 Preparation Products And Raw materials |
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