A PI3Kγ inhibitor
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CZC-24832

Item No. 14307

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-(2-amino-8-fluoro[1,2,4]triazolo[1,5-a]pyridin-6-yl)-N-(1,1-dimethylethyl)-3-pyridinesulfonamide
CAS Number
1159824-67-5
Molecular Formula
C15H17FN6O2S
Formula Weight
364.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 5 mg/mlDMSO:PBS (pH 7.2)(1:5): 0.2 mg/ml
λmax
218, 254, 292 nm
SMILES
O=S(C1=CC(C2=CN3C(C(F)=C2)=NC(N)=N3)=CN=C1)(NC(C)(C)C)=O.Cl
InChi Code
InChI=1S/C15H17FN6O2S.ClH/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);1H
InChi Key
GTDFAYLFDOPVIV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $108

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    10 mg

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    25 mg

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    50 mg

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    Product Description

    CZC-24832 is an inhibitor of PI3Kγ (IC50 = 0.025 µM in a binding assay).1 It is selective for PI3Kγ over PI3Kδ, PI3Kα, and PI3Kβ (IC50s = 7.9, >10, and 1.26 µM, respectively, in binding assays), as well as a panel of 154 lipid and protein kinases.1,2 CZC-24832 inhibits phosphorylation of Akt induced by complement component 5a (C5a) in RAW 264.7 macrophages (IC50 = 1.2 µM) and migration of isolated human granulocytes induced by fMLP (Item No. 21495; IC50 = 1 µM).2 It decreases disease severity in a mouse model of collagen-induced arthritis when administered at doses of 3 and 10 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bell, K., Sunose, M., Ellard, K., et al. SAR studies around a series of triazolopyridines as potent and selective PI3Kγ inhibitors. Bioorg. Med. Chem. Lett. 22(16), 5257-5263 (2012).

    2. Bergamini, G., Bell, K., Shimamura, S., et al. A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation. Nat. Chem. Biol. 8(6), (2012).