A PI3Kγ inhibitor
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AZD 3458

Item No. 42104

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[5-[2-[(1S)-1-cyclopropylethyl]-2,3-dihydro-7-(methylsulfonyl)-1-oxo-1H-isoindol-5-yl]-4-methyl-2-thiazolyl]-acetamide
CAS Number
2132961-46-5
Molecular Formula
C20H23N3O4S2
Formula Weight
433.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlMethanol: Sparingly soluble: 1-10 mg/ml
SMILES
CS(=O)(C1=C2C(CN(C2=O)[C@@H](C)C3CC3)=CC(C4=C(C)N=C(NC(C)=O)S4)=C1)=O
InChi Code
InChI=1S/C20H23N3O4S2/c1-10-18(28-20(21-10)22-12(3)24)14-7-15-9-23(11(2)13-5-6-13)19(25)17(15)16(8-14)29(4,26)27/h7-8,11,13H,5-6,9H2,1-4H3,(H,21,22,24)/t11-/m0/s1
InChi Key
PAQUFWFUOVDUIO-NSHDSACASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    Product Description

    AZD 3458 is an inhibitor of PI3Kγ (IC50 = 0.79 nM).1 It is selective for PI3Kγ over PI3Kα, PI3Kβ, and PI3Kδ (IC50s = 7.94, >31.62, and 0.316 µM, respectively), PI3KC2α, PI3KC2γ, and PI3KC3 (IC50s = >10, 3.16, and 7.94 µM, respectively), and a panel of 395 kinases at 1 µM but does inhibit PI3KC2β (IC50 = 31.62 nM). AZD 3458 (0.1, 0.5, and 2.5 mg/kg) reduces LPS-induced increases in the number of neutrophils in bronchoalveolar lavage fluid (BALF) in a rat model of acute lung inflammation.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Pemberton, N., Mogemark, M., Arlbrandt, S., et al. Discovery of highly isoform selective orally bioavailable phosphoinositide 3-kinase (PI3K)-γ inhibitors. J. Med. Chem. 61(12), 5435-5441 (2018).