A dual inhibitor of PI3K and mTOR
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PKI-402

Item No. 27664

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[3-ethyl-7-(4-morpholinyl)-3H-1,2,3-triazolo[4,5-d]pyrimidin-5-yl]phenyl]-N'-[4-[(4-methyl-1-piperazinyl)carbonyl]phenyl]-urea
CAS Number
1173204-81-3
Molecular Formula
C29H34N10O3
Formula Weight
570.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
SMILES
CN1CCN(C(C2=CC=C(NC(NC3=CC=C(C4=NC(N5CCOCC5)=C(N=NN6CC)C6=N4)C=C3)=O)C=C2)=O)CC1
InChi Code
InChI=1S/C29H34N10O3/c1-3-39-27-24(34-35-39)26(37-16-18-42-19-17-37)32-25(33-27)20-4-8-22(9-5-20)30-29(41)31-23-10-6-21(7-11-23)28(40)38-14-12-36(2)13-15-38/h4-11H,3,12-19H2,1-2H3,(H2,30,31,41)
InChi Key
ZAXFYGBKZSQBIV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $63

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    5 mg

    $257

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    10 mg

    $481

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    25 mg

    $1,053

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    Product Description

    PKI-402 is a dual inhibitor of PI3K and mammalian target of rapamycin (mTOR; IC50s = 1.4, 9.2, and 1.7 nM for PI3Kα, PI3Kγ, and mTOR, respectively).1 It reduces proliferation of MDA-MB-361 and PC3 cancer cells (IC50s = 8 and 21 nM, respectively) and inhibits phosphorylation of Akt in MDA-MB-361 cells (IC50 = 5 nM). PKI-402 (25, 50, and 100 mg/kg) reduces intratumor phosphorylation of Akt and tumor growth in an MDA-MB-361 mouse xenograft model. It also inhibits tumor growth in U87MG glioma and A549 lung cancer mouse xenograft models in a dose-dependent manner.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dehnhardt, C.M., Venkatesan, A.M., Delos Santos, E., et al. Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: Discovery of PKI-402. J. Med. Chem. 53(2), 798-810 (2009).

    2. Mallon, R., Hollander, I., Feldberg, L., et al. Antitumor efficacy profile of PKI-402, a dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor. Mol. Cancer Ther. 9(4), 976-984 (2010).