PKI-179 (hydrochloride)

A dual PI3K and mTOR inhibitor

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库存: 现货

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1mg

￥812.00

650.00

- +
5mg

￥3075.00

2460.00

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10mg

￥4875.00

3900.00

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货号: ajci73558
CAS: 1463510-35-1
别名:
分子式: C25H28N8O3?HCl
分子量: 525
纯度: >98%
溶解度: DMF: 2 mg/ml,DMSO: 2.5 mg/ml,DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml,Ethanol: slightly soluble
储存: Store at -20°C
库存: 现货

Background

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.