An inhibitor of PI3Kα, PI3Kβ, and PI3Kδ
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BAY-1082439

Item No. 35456

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2,3-dihydro-8-[(2R)-2-hydroxy-3-(4-morpholinyl)propoxy]-7-methoxyimidazo[1,2-c]quinazolin-5-yl]-2-methyl-3-pyridinecarboxamide
CAS Number
1375469-38-7
Molecular Formula
C25H30N6O5
Formula Weight
494.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
227, 275 nm
SMILES
COC1=C2C(C3=NCCN3C(NC(C4=C(N=CC=C4)C)=O)=N2)=CC=C1OC[C@H](O)CN5CCOCC5
InChi Code
InChI=1S/C25H30N6O5/c1-16-18(4-3-7-26-16)24(33)29-25-28-21-19(23-27-8-9-31(23)25)5-6-20(22(21)34-2)36-15-17(32)14-30-10-12-35-13-11-30/h3-7,17,32H,8-15H2,1-2H3,(H,28,29,33)/t17-/m1/s1
InChi Key
JGNRMIWLBBNSMU-QGZVFWFLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

    $97

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    10 mg

    $152

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    25 mg

    $241

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    Product Description

    BAY-1082439 is an inhibitor of PI3Kα, PI3Kβ, and PI3Kδ (IC50s = 5, 15, and 1 nM, respectively).1 It is selective for PI3Kα, -β, and -δ over PI3Kγ (IC50 = 52 nM). BAY-1082439 selectively inhibits proliferation of PTEN-null LNCaP and PC3 prostate cancer cells over wild-type PTEN isogenic PC3 cells. BAY-1082439 (75 mg/kg) decreases intratumoral levels of phosphorylated Akt and reduces tumor growth in a mouse model of castration-resistant prostate cancer using castrated Pten conditional knockout mice (Pten-null mice). Intermittent administration of BAY-1082439 (180 mg/kg) reverses resistance to an anti-PD-1 antibody and induces CD8+ T cell clonal expansion and T cell-mediated inflammation in the tumor microenvironment in castrated Pten-null mice.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zou, Y., Qi, Z., Guo, W., et al. Cotargeting the cell-intrinsic and microenvironment pathways of prostate cancer by PI3Kα/β/δ inhibitor BAY1082439. Mol. Cancer Ther. 17(10), 2091-2099 (2018).

    2. Qi, J., Xu, Z., Zhang, L., et al. Overcoming resistance to immune checkpoint therapy in PTEN-null prostate cancer by intermittent anti-PI3Kα/β/δ treatment. Nat. Commun. 13(1), 182 (2022).