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PKI-179

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Catalog No. T36084Cas No. 1197160-28-3

PKI-179 is a potent, orally active compound that functions as a dual PI3K/mTOR inhibitor. It demonstrates IC50 values of 8 nM for PI3K-α, 24 nM for PI3K-β, 74 nM for PI3K-γ, 77 nM for PI3K-δ, and 0.42 nM for mTOR. Additionally, it is effective against E545K and H1047R mutations, with IC50s of 14 nM and 11 nM, respectively. In vivo studies have shown that PKI-179 possesses anti-tumor capabilities[1][2].

PKI-179
Other Forms of PKI-179:
PKI-179 hydrochlorideT360851463510-35-1
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PKI-179

😃Good
Catalog No. T36084Cas No. 1197160-28-3
PKI-179 is a potent, orally active compound that functions as a dual PI3K/mTOR inhibitor. It demonstrates IC50 values of 8 nM for PI3K-α, 24 nM for PI3K-β, 74 nM for PI3K-γ, 77 nM for PI3K-δ, and 0.42 nM for mTOR. Additionally, it is effective against E545K and H1047R mutations, with IC50s of 14 nM and 11 nM, respectively. In vivo studies have shown that PKI-179 possesses anti-tumor capabilities[1][2].
Pack SizePriceAvailabilityQuantity
25 mg$7676-8 weeks
50 mg$9976-8 weeks
100 mg$1,6106-8 weeks
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Product Introduction

Bioactivity
Description
PKI-179 is a potent, orally active compound that functions as a dual PI3K/mTOR inhibitor. It demonstrates IC50 values of 8 nM for PI3K-α, 24 nM for PI3K-β, 74 nM for PI3K-γ, 77 nM for PI3K-δ, and 0.42 nM for mTOR. Additionally, it is effective against E545K and H1047R mutations, with IC50s of 14 nM and 11 nM, respectively. In vivo studies have shown that PKI-179 possesses anti-tumor capabilities[1][2].
Targets&IC50
mTOR:0.42 nM (IC50), PI3Kγ:74 nM (IC50), PI3Kβ:24 nM (IC50), E545K:14 nM (IC50), PI3Kα:8 nM (IC50), H1047R:11 nM (IC50), PI3Kδ:77 nM (IC50)
In vitro
PKI-179 inhibits cell proliferation with IC50s of 22 nM and 29 nM for MDA361 and PC3 cells, respectively[1]. It shows inhibitory activity against a panel of 361 other kinases, hERG, and cytochrome P450 (CYP) isoforms at concentrations up to >30 μM, but remains active for CYP2C8 (IC50=3 μM)[1].
In vivo
PKI-179 (5-50 mg/kg; p.o. once daily for 40 days) inhibits tumor growth and is well tolerated in nude mice bearing MDA-361 human breast cancer tumors. PKI-179 (50 mg/kg; p.o.) effectively inhibits PI3K signaling in nude mice with MDA361 tumor xenografts. PKI-179 demonstrates good oral bioavailability (98% in nude mouse, 46% in rat, 38% in monkey, and 61% in dog) and a high half-life (>60 min) [1].
Chemical Properties
Molecular Weight488.54
FormulaC25H28N8O3
Cas No.1197160-28-3
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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Keywords

PKI179PKI 179PKI-179
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