A dual inhibitor of PI3K and mTOR
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PF-04979064

Item No. 39527

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1,3-dihydro-1-[1-[(2S)-2-hydroxy-1-oxopropyl]-4-piperidinyl]-3-methyl-8-(6-methyl-3-pyridinyl)-2H-imidazo[4,5-c][1,5]naphthyridin-2-one
CAS Number
1220699-06-8
Molecular Formula
C24H26N6O3
Formula Weight
446.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Methanol: Soluble
λmax
272, 325 nm
SMILES
O=C1N(C2CCN(CC2)C([C@H](C)O)=O)C3=C(N1C)C=NC4=CC=C(C5=CN=C(C=C5)C)N=C34
InChi Code
InChI=1S/C24H26N6O3/c1-14-4-5-16(12-25-14)18-6-7-19-21(27-18)22-20(13-26-19)28(3)24(33)30(22)17-8-10-29(11-9-17)23(32)15(2)31/h4-7,12-13,15,17,31H,8-11H2,1-3H3/t15-/m0/s1
InChi Key
GACQNUHFDBEIQH-HNNXBMFYSA-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

    PF-04979064 is a dual inhibitor of PI3K and mTOR (Kis = 0.13, 0.111, 0.122, and 1.42 nM for PI3Kα, PI3Kγ, PI3Kδ, and mTOR, respectively).1 It is selective for PI3K and mTOR over a panel of 36 other kinases at 1 µM. PF-04979064 inhibits phosphorylation of Akt in BT-20 breast cancer cells (IC50 = 9.1 nM). It reduces tumor volume by 88% in a U87MG glioblastoma mouse xenograft model when administered at a dose of 40 mg/kg. PF-04979064 also increases alveolar epithelial cell apoptosis in a mouse model of chronic obstructive pulmonary disease (COPD) induced by fine particulate matter less than 2.5 µm (PM2.5).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cheng, H., Li, C., Bailey, S., et al. Discovery of the highly potent PI3K/mTOR dual inhibitor PF-04979064 through structure-based drug design. ACS Med. Chem. Lett. 4(1), 91-97 (2012).

    2. Zhang, F., Ma, H., Wang, Z.L., et al. The PI3K/AKT/mTOR pathway regulates autophagy to induce apoptosis of alveolar epithelial cells in chronic obstructive pulmonary disease caused by PM2.5 particulate matter. J. Int. Med. Res. 48(7), 300060520927919 (2020).