A PI3Kα inhibitor
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CNX-1351

Item No. 30264

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[4-[[2-(1H-indazol-4-yl)-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-6-yl]methyl]-1-piperazinyl]-6-methyl-5-heptene-1,4-dione
CAS Number
1276105-89-5
Molecular Formula
C30H35N7O3S
Formula Weight
573.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml
λmax
216, 320 nm
SMILES
C/C(C)=C/C(CCC(N1CCN(CC2=CC3=NC(C4=C(C=NN5)C5=CC=C4)=NC(N6CCOCC6)=C3S2)CC1)=O)=O
InChi Code
InChI=1S/C30H35N7O3S/c1-20(2)16-21(38)6-7-27(39)36-10-8-35(9-11-36)19-22-17-26-28(41-22)30(37-12-14-40-15-13-37)33-29(32-26)23-4-3-5-25-24(23)18-31-34-25/h3-5,16-18H,6-15,19H2,1-2H3,(H,31,34)
InChi Key
DLNUPKDFXMWRFP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    CNX-1351 is a covalent inhibitor of PI3Kα (IC50 = 6.8 nM).1 It is selective for PI3Kα over PI3Kβ, -γ, and -δ (IC50s = 166, 240.3, and 3,020 nM, respectively), as well as PI3KC2A, PI3KC, PI4Kα, PI4Kβ, SPHK1, and SPHK2 (IC50s = >1 µM for all). CNX-1351 (500 nM) inhibits phosphorylation of Akt in SKOV3 cells. It inhibits the growth of SKOV3 and MCF-7 cancer cells (GI50s = 77.6 and 54.7 nM, respectively). CNX-1351 (100 mg/kg) inhibits Akt phosphorylation in mouse spleen.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Nacht, M., Qiao, L., Sheets, M.P., et al. Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα. J. Med. Chem. 56(3), 712-721 (2013).