A dual PI3K and mTOR inhibitor
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PKI-179 (hydrochloride)

Item No. 21202

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[4-(4-morpholinyl)-6-(3-oxa-8-azabicyclo[3.2.1]oct-8-yl)-1,3,5-triazin-2-yl]phenyl]-N'-4-pyridinyl-urea, monohydrochloride
CAS Number
1463510-35-1
Molecular Formula
C25H28N8O3 • HCl
Formula Weight
525.0
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMSO: 2.5 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.25 mg/mlEthanol: slightly soluble
λmax
228, 297 nm
SMILES
O=C(NC1=CC=C(C2=NC(N3CCOCC3)=NC(N4C5COCC4CC5)=N2)C=C1)NC6=CC=NC=C6.Cl
InChi Code
InChI=1S/C25H28N8O3.ClH/c34-25(28-19-7-9-26-10-8-19)27-18-3-1-17(2-4-18)22-29-23(32-11-13-35-14-12-32)31-24(30-22)33-20-5-6-21(33)16-36-15-20;/h1-4,7-10,20-21H,5-6,11-16H2,(H2,26,27,28,34);1H
InChi Key
JNMURGIZAFELTR-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

    PKI-179 is an orally bioavailable dual inhibitor of PI3K and mammalian target of rapamycin (mTOR).1 In an in vitro enzymatic assay, it potently inhibits PI3K (IC50s = 8, 24, 17, and 74 nM for isoforms α, β, δ, and γ, respectively), two common PI3Kα mutants, E545K and H1047R (IC50s = 14 and 11 nM, respectively), and mTOR (IC50 = 0.42 nM). PKI-179 is selective for PI3K and mTOR over a panel of 361 other kinases at IC50 values up to 50 μM, hERG (IC50 > 30 μM), and cytochrome P450 (CYP) isoforms (IC50s > 30 μM), but does have activity for CYP2C8 (IC50 = 3 μM). It inhibits proliferation through the Akt/mTOR signaling pathway in MDA-361 breast and PC3MM2 prostate cancer cell lines in vitro (IC50s = 22 and 29 nM, respectively) and inhibits tumor growth in an MDA-361 mouse xenograft model when used at a dose of 50 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Venkatesan, A.M., Chen, Z., dos Santos, O., et al. PKI-179: An orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor. Bioorg. Med. Chem. Lett. 20(19), 5869-5873 (2010).