PKI-179 (hydrochloride) |
カタログ番号GC44658 |
PKI-179 (塩酸塩) は、PI3K-α、PI3K-β、PI3K-γ、PI3K に対する IC50 が 8 nM、24 nM、74 nM、77 nM、および 0.42 nM である、強力で経口的に活性なデュアル PI3K/mTOR 阻害剤です。それぞれ-δとmTOR。 PKI-179 (塩酸塩) も、E545K および H1047R に対して活性を示し、IC50 はそれぞれ 14 nM および 11 nM です。 PKI-179 (塩酸塩) は、in vivo で抗腫瘍活性を示します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1463510-35-1
Sample solution is provided at 25 µL, 10mM.
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.
Average Rating: 5
(Based on Reviews and 19 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *