1. PI3K/Akt/mTOR
  2. PI3K
    mTOR
  3. PKI-179 hydrochloride

PKI-179 hydrochloride 

Cat. No.: HY-11080A Purity: 98.11%
Handling Instructions

PKI-179 hydrochloride is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 hydrochloride also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride shows anti-tumor activity in vivo.

For research use only. We do not sell to patients.

PKI-179 hydrochloride Chemical Structure

PKI-179 hydrochloride Chemical Structure

CAS No. : 1463510-35-1

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Solution
10 mM * 1 mL USD 289 In-stock
Estimated Time of Arrival: December 31
Solid
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10 mg USD 400 In-stock
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25 mg USD 800 In-stock
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50 mg USD 1280 In-stock
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100 mg USD 1950 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

PKI-179 hydrochloride is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 hydrochloride also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride shows anti-tumor activity in vivo[1][2].

IC50 & Target[1]

mTOR

0.42 nM (IC50)

PI3Kα

8 nM (IC50)

PI3Kβ

24 nM (IC50)

PI3Kγ

74 nM (IC50)

PI3Kδ

77 nM (IC50)

E545K

14 nM (IC50)

H1047R

77 nM (IC50)

In Vitro

PKI-179 inhibits the cell proliferation, with IC50s of 22 nM and 29 nM for MDA361 and PC3 cells, respectively[1].
PKI-179 shows inhibitory activity against a panel of 361 other kinases, hERG and cytochrome P450 (CYP) isoforms at concentrations up to >30 μM, but does have activity for CYP2C8 (IC50=3 μM)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PKI-179 (5-50 mg/kg; p.o. once daily for 40 days) inhibits the tumor growth and is well tolerated in nude mice bearing MDA-361 human breast cancer tumors[1].
PKI-179 (50 mg/kg; p.o.) results in good inhibition of PI3K signaling in nude mice bearing MDA361 tumor xenografts[1].
PKI-179 exhibits 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice bearing MDA-361 human breast cancer tumors[1]
Dosage: 5, 10, 25, 50 mg/kg
Administration: I.p. every 3 days for 4 weeks
Result: Exhibited pronounced tumor growth arrest when dosed above 10 mg/kg.
No significant weight loss of tested animals was observed for all different dosages.
Molecular Weight

525.00

Formula

C₂₅H₂₉ClN₈O₃

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
References
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PKI-179 hydrochloride
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HY-11080A
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