| Bioactivity | CZC24832 is a highly selective and potent PI3Kγ inhibitor (IC50=27 nM) with apparent dissociation constants (Kdapp) of 19 nM. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | CZC24832 | ||||||||||||
| CAS | 1159824-67-5 | ||||||||||||
| Formula | C15H17FN6O2S | ||||||||||||
| Molar Mass | 364.40 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Bergamini G, et al. A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation. Nat Chem Biol. 2012 Apr 29;8(6):576-82. |
CZC24832
CAS: 1159824-67-5 F: C15H17FN6O2S W: 364.40
CZC24832 is a highly selective and potent PI3Kγ inhibitor (IC50=27 nM) with apparent dissociation constants (Kdapp) of
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