A dual PI3K and mTOR inhibitor; inhibits PI3K (IC50s = 8

PKI-179 (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
1463510-35-1
Storage:
-20
UN-No:
Non-Hazardous - /

PKI-179 is an orally bioavailable dual inhibitor of PI3K and mammalian target of rapamycin (mTOR).{39367} 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.  

 

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Description

A dual PI3K and mTOR inhibitor; inhibits PI3K (IC50s = 8, 24, 17, and 74 nM for isoforms α, β, δ, and γ, respectively); inhibits PI3Kα mutants, E545K and H1047R (IC50s = 14 and 11 nM, respectively); inhibits mTOR (IC50 = 0.42 nM); antiproliferative against MDA-361 (breast) and PC3MM2 (prostate) cell lines (IC50s = 22 and 29 nM, respectively); inhibits tumor growth in MDA-361 mouse xenografts (50 mg/kg)

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

Synonyms: 

Molecular weight: 525

CAS: 1463510-35-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|mTOR||Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling

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