Potent, cell permeable PI3K inhibitor
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PIK-90

Item No. 10010749

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(2,3-dihydro-7,8-dimethoxyimidazo[1,2-c]quinazolin-5-yl)-3-pyridinecarboxamide
CAS Number
677338-12-4
Synonyms
  • PIK-85
Molecular Formula
C18H17N5O3
Formula Weight
351.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 0.5 mg/ml
λmax
229, 276 nm
SMILES
COC1=CC=C2C(N=C(NC(C3=CN=CC=C3)=O)N4C2=NCC4)=C1OC
InChi Code
InChI=1S/C18H17N5O3/c1-25-13-6-5-12-14(15(13)26-2)21-18(23-9-8-20-16(12)23)22-17(24)11-4-3-7-19-10-11/h3-7,10H,8-9H2,1-2H3,(H,21,22,24)
InChi Key
ZJAVHOMVDCMAMF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $21

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    5 mg

    $69

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    10 mg

    $95

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    Cayman Chemical
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    Product Description

    PIK-90 is a potent and cell permeable phosphoinositide 3-kinase (PI3K) inhibitor (IC50 = 11, 350, 18, and 58 nM for p110 subunit isoforms α, β, γ, and δ, respectively).1 Through this action, PIK-90 reduces chemotaxis and induces apoptosis in chronic lymphocytic leukemia B cells.1 It also blocks proliferation of glioma cells in vitro.2 By inhibiting P110α, PIK-90 blocks insulin-stimulated phosphorylation of Akt in L1 adipocytes and L6 myotubes, preventing activation of the mTORC1 pathway.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Niedermeier, M., Hennessy, B.T., Knight, Z.A., et al. Isoform-selective phosphoinositide 3'-kinase inhibitors inhibit CXCR4 signaling and overcome stromal cell-mediated drug resistance in chronic lymphocytic leukemia: A novel therapeutic approach. Blood 113(22), 5549-5557 (2009).

    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).

    3. 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).