PKI-179 (hydro<wbr/>chloride)

PKI-179 (hydrochloride)

CAT N°: 21202
Price:

From 92.00 78.20

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 ?, ?, ?, and ?, respectively), two common PI3K? 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 ?M, hERG (IC50 > 30 ?M), and cytochrome P450 (CYP) isoforms (IC50s > 30 ?M), but does have activity for CYP2C8 (IC50 = 3 ?M). 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.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 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
  • Correlated keywords
    • 1197160-28-3 PKI179 phosphatidylinositol-3 phosphoinositide 1634621-81-0 PI3Ka E-545K H-1047R CYP450 CYP-2C8 MDA361 PC3-MM2 human Ether-à-go-go-Related Gene antiproliferative anti-proliferative
  • Product Overview:
    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 ?, ?, ?, and ?, respectively), two common PI3K? 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 ?M, hERG (IC50 > 30 ?M), and cytochrome P450 (CYP) isoforms (IC50s > 30 ?M), but does have activity for CYP2C8 (IC50 = 3 ?M). 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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