A PI3Kβ/δ inhibitor
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AZD 8186

Item No. 17384

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
8-[(1R)-1-[(3,5-difluorophenyl)amino]ethyl]-N,N-dimethyl-2-(4-morpholinyl)-4-oxo-4H-1-benzopyran-6-carboxamide
CAS Number
1627494-13-6
Molecular Formula
C24H25F2N3O4
Formula Weight
457.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: 2 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 0.5 mg/ml
λmax
219, 242, 311 nm
SMILES
FC1=CC(F)=CC(N[C@H](C)C2=C(OC(N3CCOCC3)=CC4=O)C4=CC(C(N(C)C)=O)=C2)=C1
InChi Code
InChI=1S/C24H25F2N3O4/c1-14(27-18-11-16(25)10-17(26)12-18)19-8-15(24(31)28(2)3)9-20-21(30)13-22(33-23(19)20)29-4-6-32-7-5-29/h8-14,27H,4-7H2,1-3H3/t14-/m1/s1
InChi Key
LMJFJIDLEAWOQJ-CQSZACIVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $128

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    10 mg

    $169

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    25 mg

    $378

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    Product Description

    AZD 8186 is a selective PI3Kβ/δ inhibitor that exhibits IC50 values of 3, 17, and 752 nM for PI3Kβ, δ, and α, respectively, in cells sensitive to isoform-specific PI3K inhibition.1,2 It shows no significant binding against a panel of 442 other kinases when tested at a concentration of 10 µM and exhibits high oral efficacy in mouse cancer models.1 AZD 8186 inhibits growth of a range of cell lines, with preferential activity in cells with PTEN mutation or deficiency, and inhibits growth of prostate and triple negative breast cancer tumors in vivo, both as a single agent and in combination with docetaxel (Item No. 11637).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Barlaam, B., Cosulich, S., Degorce, S., et al. Discovery of (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): A potent and selective inhibitor of PI3Kβ and PI3Kδ for the treatment of PTEN-deficient cancers. J. Med. Chem. 58(2), 943-962 (2015).

    2. Hancox, U., Cosulich, S., Hanson, L., et al. Inhibition of PI3Kβ signaling with AZD8186 inhibits growth of PTEN-deficient breast and prostate tumors alone and in combination with docetaxel. Mol. Cancer Ther. 14(1), 48-58 (2015).