An inhibitor of PI3Kα and PI3Kδ
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AZD 8835

Item No. 29166

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[4-[5-[5-amino-6-[5-(1,1-dimethylethyl)-1,3,4-oxadiazol-2-yl]-2-pyrazinyl]-1-ethyl-1H-1,2,4-triazol-3-yl]-1-piperidinyl]-3-hydroxy-1-propanone
CAS Number
1620576-64-8
Molecular Formula
C22H31N9O3
Formula Weight
469.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 16 mg/mlDMSO: 16 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 2 mg/ml
λmax
235, 289, 378 nm
SMILES
O=C(CCO)N1CCC(C2=NN(CC)C(C3=CN=C(N)C(C4=NN=C(C(C)(C)C)O4)=N3)=N2)CC1
InChi Code
InChI=1S/C22H31N9O3/c1-5-31-19(26-18(29-31)13-6-9-30(10-7-13)15(33)8-11-32)14-12-24-17(23)16(25-14)20-27-28-21(34-20)22(2,3)4/h12-13,32H,5-11H2,1-4H3,(H2,23,24)
InChi Key
ZGRDYKFVDCFJCZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $128

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    10 mg

    $235

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    25 mg

    $487

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    Product Description

    AZD 8835 is an inhibitor of PI3Kα and PI3Kδ (IC50s = 6.2 and 5.7 nM, respectively).1 It is selective for PI3Kα and PI3Kδ over PI3Kβ and PI3Kγ (IC50s = 431 and 90 nM, respectively). AZD 8835 inhibits Akt phosphorylation in PIK3CA constitutively active mutant BT474 cells and Jeko-1 B cells that express endogenous PI3Kδ (IC50s = 57 and 49 nM, respectively). In vivo, AZD 8835 (25 mg/kg) reduces tumor growth and Akt phosphorylation in a SKOV3 mouse xenograft model. It also increases the activity of CD8+ effector T cells and reduces tumor growth in a C26 mouse syngeneic tumor model.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Barlaam, B., Cosulich, S., Delouvrié, B., et al. Discovery of 1-(4-(5-(5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one (AZD8835): A potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment of cancers. Bioorg. Med. Chem. Lett. 25(22), 5155-5162 (2015).

    2. Carnevalli, L.S., Sinclair, C., Taylor, M.A., et al. PI3Kα/δ inhibition promotes anti-tumor immunity through direct enhancement of effector CD8+ T-cell activity. J. Immunother. Cancer 6(1), 158 (2018).