PI3K/mTOR Inhibitor-11

PI3K/mTOR Inhibitor-11 is an orally active PI3K/mTOR inhibitor ( IC 50 : 3.5, 4.6, and 21.3 nM for PI3Kα , PI3Kδ , and mTOR). PI3K/mTOR Inhibitor-11 regulates the PI3K/AKT/mTOR signaling pathway by inhibiting the phosphorylation of AKT and S6 proteins. PI3K/mTOR Inhibitor-11 can be used in the research of cancers In Vitro PI3K/mTOR Inhibitor-11 (compound 8o) inhibits various human cancer cell lines HT29, HCT15, H3122, HeLa, SW620, and H446 viability with IC 50 values of 0.25, 0.17, 0.29, 0.09, 0.16, and 0.97 μM, respectively. PI3K/mTOR Inhibitor-11 (0-1.25 μM, 15 days) decreases the colony formation rates of HeLa and SW620 cells. PI3K/mTOR Inhibitor-11 (0-2.5 μM, 24 h) arrests HeLa and SW620 cells at the G0/G1 phases. PI3K/mTOR Inhibitor-11 (0-2.5 μM, 24 h) suppressees the phosphorylated AKT and S6 proteins in HeLa cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell Line: HeLa and SW620 cells Concentration: 0, 0.15625, 0.625, 1.25 μM Incubation Time: 24 h Result: Affected HeLa cells’ apoptosis rate from 6.10 to 66.04% in a dose-dependent manner. Western Blot AnalysisCell Line: HeLa Concentration: 0, 0.15625, 0.625, 1.25, 2.5 μM Incubation Time: 24 h Result: Suppressed the phosphorylated AKT (Ser473 and Thr308) and S6 proteins. In Vivo PI3K/mTOR Inhibitor-11 (compound 8o, 15-60 mg/kg, intragastric administration) suppresses the growth of HeLa and SW620 xenograft tumors . PI3K/mTOR Inhibitor-11 (1 mg/kg for i.v., 10 mg/kg for p.o., rats) shows oral bioavailability (76.81%) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: HeLa and SW620 xenograft models of female BALB/c nude mice . Dosage: 15, 30, and 60 mg/kg Administration: Intragastric administration, daily for 30 days. Result: The TGIs (tumor growth inhibitions): 80.22, 73.50, and 60.79% in the HeLa xenograft model at doses of 60, 30, and 15 mg/kg, respectively. TGIs: 81.03, 70.81, and 60.58% in the SW620 xenograft model at doses of 60, 30, and 15 mg/kg, respectively. Animal Model: Rats . Dosage: 1 mg/kg for i.v., 10 mg/kg for p.o. Administration: i.v., p.o. Result: Pharmacokinetic parameters of PI3K/mTOR Inhibitor-11 (compound 8o) dose (mg/kg) T 1/2 (h) C max (ng/mL) CL (mL/min/kg) F (%) 1 (i.v.) 17.2 10 (p.o.) 2.6 2995 76.81% Form:Solid IC50& Target:PI3Kα 3.5 nM (IC 50 ) PI3Kδ 4.6 nM (IC 50 ) mTOR 21.3 nM (IC 50 )

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