A potent, cell-permeable PI3K inhibitor
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Alternative(s)
10009209PI-103
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PI-103 (hydrochloride)

Item No. 21187

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[4-(4-morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]-phenol, monohydrochloride
CAS Number
371935-79-4
Molecular Formula
C19H16N4O3 • HCl
Formula Weight
384.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 5 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml
λmax
211, 288, 319 nm
SMILES
OC1=CC(C2=NC(N3CCOCC3)=C(OC4=NC=CC=C45)C5=N2)=CC=C1.Cl
InChi Code
InChI=1S/C19H16N4O3.ClH/c24-13-4-1-3-12(11-13)17-21-15-14-5-2-6-20-19(14)26-16(15)18(22-17)23-7-9-25-10-8-23;/h1-6,11,24H,7-10H2;1H
InChi Key
XSQMYBFFYPTMFE-UHFFFAOYSA-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

    PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of PI3K family members with selectivity toward DNA-PK, PI3K (p110α), and mTORC1. The IC50 values are 2, 8, 20, 26, 48, 83, 88, and 150 nM for DNA-PK, p110α, mTORC1, PI3-KC2β, p110δ, mTORC2, p110β, and p110γ, respectively.1 PI-103 exhibits antiproliferative activity against a panel of glioma cell lines in vitro at a concentration of 0.5 µM. It also inhibits growth of established human glioma tumor xenografts in vivo with no observable toxicity.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Knight, Z.A., Gonzalez, B., Feldman, M.E., et al. A pharmacological map of the PI3-K family defines a role for p110α in insulin signaling. Cell 125(4), 733-747 (2006).

    2. Fan, Q.W., Knight, Z.A., Goldenberg, D.D., et al. A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer Cell 9(5), 341-349 (2006).