A potent, dual PI3K/mTOR inhibitor
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PF-05212384

Item No. 14567

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[[4-(dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N'-[4-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)phenyl]-urea
CAS Number
1197160-78-3
Synonyms
  • PK-1587
  • PKI-587
Molecular Formula
C32H41N9O4
Formula Weight
615.7
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1.5 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 1 mg/ml
λmax
228, 303 nm
SMILES
O=C(N1CCC(N(C)C)CC1)C2=CC=C(NC(NC3=CC=C(C4=NC(N5CCOCC5)=NC(N6CCOCC6)=N4)C=C3)=O)C=C2
InChi Code
InChI=1S/C32H41N9O4/c1-38(2)27-11-13-39(14-12-27)29(42)24-5-9-26(10-6-24)34-32(43)33-25-7-3-23(4-8-25)28-35-30(40-15-19-44-20-16-40)37-31(36-28)41-17-21-45-22-18-41/h3-10,27H,11-22H2,1-2H3,(H2,33,34,43)
InChi Key
DWZAEMINVBZMHQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    Product Description

    Phosphatidylinositol-3-kinases (PI3Ks) act in concert with mTOR complexes to regulate signaling pathways that have critical roles in cancer and other diseases.1,2 PF-05212384 is a potent, dual PI3K/mTOR inhibitor (IC50 values are 0.4 and 5.4 nM for PI3Kα and PI3Kγ, respectively, and 1.6 nM for mTOR).3,4 It is active both in vitro and in vivo, inhibiting the growth of cancer cells in culture or in xenografts in mice when delivered intravenously.3,4 PF-05212384 blocks the proliferation of liver cancer stem cells, and this effect is enhanced in combination therapy with the multikinase inhibitor BAY-43-9006 (Item No. 10009644).5 PF-05212384 action also enhances the effectiveness of cetuximab or radiation therapy in human head and neck cancer models.6,7

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Petroulakis, E., Mamane, Y., Le Bacquer, O., et al. mTOR signaling: implications for cancer and anticancer therapy. Br. J. Cancer 94(2), 195-199 (2006).

    2. Liu, P., Cheng, H., Roberts, T.M., et al. Targeting the phosphoinositide 3-kinase (PI3K) pathway in cancer. Nat. Rev. Drug Discov. 8(8), 627-644 (2009).

    3. Mallon, R., Feldberg, L.R., Lucas, J., et al. Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor. Clin. Cancer Res. 17(10), 3193-3203 (2011).

    4. Venkatesan, A.M., Dehnhardt, C.M., Delos Santos, E., et al. Bis(morpholino-1,3,5-triazine) derivatives: Potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: Discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor. J. Med. Chem. 53(6), 2636-2645 (2010).

    5. Gedaly, R., Galuppo, R., Musgrave, Y., et al. PKI-587 and sorafenib alone and in combination on inhibition of liver cancer stem cell proliferation. J. Surg. Res. 185(1), 225-230 (2013).

    6. D'Amato, V., Rosa, R., D'Amato, C., et al. The dual PI3K/mTOR inhibitor PKI-587 enhances sensitivity to cetuximab in EGFR-resistant human head and neck cancer models. Br. J. Cancer 110(12), 2887-2895 (2014).

    7. Leiker, A.J., DeGraff, W., Choudhuri, R., et al. Radiation enhancement of head and neck squamous cell carcinoma by the dual PI3K/mTOR inhibitor PF-05212384. Clin. Cancer Res. 21(12), 2792-2801 (2015).