Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
25 mg | 約6-8 週間 | ¥ 176,000 |
50 mg | 約6-8 週間 | ¥ 229,000 |
100 mg | 約6-8 週間 | ¥ 369,500 |
説明 | 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. |
ターゲット&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) |
分子量 | 525 |
分子式 | C25H29ClN8O3 |
CAS No. | 1463510-35-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: Slightly soluble
DMF: 2 mg/mL
DMSO:PBS(pH 7.2) (1:3): 0.25 mg/mL
DMSO: 2.5 mg/mL
You can also refer to dose conversion for different animals. 詳細
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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.
PKI-179 hydrochloride 1463510-35-1 PKI 179 Hydrochloride PKI179 hydrochloride PKI179 Hydrochloride PKI 179 hydrochloride PKI-179 Hydrochloride Inhibitor inhibitor inhibit