A potent inhibitor of p110δ
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PIK-294

Item No. 23427

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[4-amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone
CAS Number
900185-02-6
Molecular Formula
C28H23N7O2
Formula Weight
489.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:6): 0.14 mg/mlEthanol: 0.25 mg/ml
λmax
205, 271 nm
SMILES
O=C1N(C(CN2C3=NC=NC(N)=C3C(C4=CC=CC(O)=C4)=N2)=NC5=CC=CC(C)=C15)C6=C(C)C=CC=C6
InChi Code
InChI=1S/C28H23N7O2/c1-16-7-3-4-12-21(16)35-22(32-20-11-5-8-17(2)23(20)28(35)37)14-34-27-24(26(29)30-15-31-27)25(33-34)18-9-6-10-19(36)13-18/h3-13,15,36H,14H2,1-2H3,(H2,29,30,31)
InChi Key
WFSLJOPRIJSOJR-UHFFFAOYSA-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

    $236

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    25 mg

    $502

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    Product Description

    PIK-294 is a potent inhibitor of the phosphatidylinositol 3-kinase (PI3K) catalytic subunit p110δ (IC50s = 10,000, 490, 10, and 160 nM, for p110 subunit isoforms α, β, δ, and γ, respectively).1 It is selective for PI3K p110 subunit isoforms over DNA-PK, mTOR, and eight tyrosine kinases tested.2 It inhibits chemokinetic and chemotactic migration of neutrophils induced by CXCL8 in a three-dimensional collagen gel migration assay.3

    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. Apsel, B., Blair, J.A., Gonzalez, B., et al. Targeted polypharmacology: Discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat. Chem. Biol. 4(11), 691-699 (2008).

    3. Martin, K.J.S., Muessel, M.J., Pullar, C.E., et al. The role of phosphoinositide 3-kinases in neutrophil migration in 3D collagen gels. PLoS One 10(2), e0116250 (2015).