A selective inhibitor of PI3Kα
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GDC-0326

Item No. 19241

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2S)-2-[[5,6-dihydro-2-[1-(1-methylethyl)-1H-1,2,4-triazol-5-yl]imidazo[1,2-d][1,4]benzoxazepin-9-yl]oxy]-propanamide
CAS Number
1282514-88-8
Molecular Formula
C19H22N6O3
Formula Weight
382.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: Slightly soluble
λmax
276, 306 nm
SMILES
O=C(N)[C@H](C)OC1=CC=C(C2=NC(C3=NC=NN3C(C)C)=CN2CCO4)C4=C1
InChi Code
InChI=1S/C19H22N6O3/c1-11(2)25-19(21-10-22-25)15-9-24-6-7-27-16-8-13(28-12(3)17(20)26)4-5-14(16)18(24)23-15/h4-5,8-12H,6-7H2,1-3H3,(H2,20,26)/t12-/m0/s1
InChi Key
SIKYDKLGPWRPMZ-LBPRGKRZSA-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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    Product Description

    GDC-0326 is an inhibitor of phosphatidylinositol 3-kinase α (PI3Kα; Ki = 0.2 nM) that is 133-, 20-, and 51-fold selective for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively.1 It inhibits proliferation of MCF7-neo/HER2 and PC3 cells (EC50s = 0.1 and 2.2 μM, respectively). In vivo, GDC-0326 (6.25 mg/kg) induces tumor regression in a KPL-4 mouse xenograft model. It also reduces tumor growth, tumor vasculature, and the number of liver and lymph node metastases in the RIP1-Tag2 transgenic mouse model of pancreatic neuroendocrine tumors.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Heffron, T.P., Heald, R.A., Ndubako, C.O., et al. The rational design of selective benzoxazepin inhibitors of the α-isoform of phosphoinositide 3-kinase culminating in the identification of (S)-2-((2-(1-isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326). J. Med. Chem. 59(3), 985-1002 (2016).

    2. Soler, A., Figueiredo, A.M., Castel, P., et al. Therapeutic benefit of selective inhibition of p110α PI3-kinase in pancreatic neuroendocrine tumors. Clin. Cancer Res. 22(23), 5805-5817 (2016).