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PKI-179 hydrochloride

Catalog No. T36085 CAS 1463510-35-1

PKI-179 is an orally bioavailable dual inhibitor of PI3K and mammalian target of rapamycin (mTOR). 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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PKI-179 hydrochloride Chemical Structure

PKI-179 hydrochloride, CAS 1463510-35-1

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 767.00
50 mg	6-8 weeks	$ 997.00
100 mg	6-8 weeks	$ 1,610.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description

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

Targets&IC50

mTOR:0.42 nM (IC50), PI3Kγ:74 nM (IC50), H1047R:77 nM (IC50), PI3Kα:8 nM (IC50), E545K:14 nM (IC50), PI3Kβ:24 nM (IC50), PI3Kδ:77 nM (IC50)

Molecular Weight	525
Formula	C25H29ClN8O3
CAS No.	1463510-35-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: Slightly soluble

DMF: 2 mg/mL

DMSO:PBS(pH 7.2) (1:3): 0.25 mg/mL

DMSO: 2.5 mg/mL

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PKI-179 hydrochloride 1463510-35-1 PKI 179 Hydrochloride PKI179 hydrochloride PKI179 Hydrochloride PKI 179 hydrochloride PKI-179 Hydrochloride inhibitor inhibit

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