产品
编 号：F756319
分子式：C27H21N7
分子量：443.5
分子式：C27H21N7
分子量：443.5
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2845104-25-6
产品详情
生物活性：
PI3K/mTOR Inhibitor-11 is an orally active PI3K/mTOR inhibitor (IC50: 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.
体内研究：
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%).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)T1/2 (h)Cmax (ng/mL) CL (mL/min/kg)F (%)
1 (i.v.)17.2
10 (p.o.)2.6299576.81%
体外研究：
PI3K/mTOR Inhibitor-11 (compound 8o) inhibits various human cancer cell lines HT29, HCT15, H3122, HeLa, SW620, and H446 viability with IC50 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.
PI3K/mTOR Inhibitor-11 is an orally active PI3K/mTOR inhibitor (IC50: 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.
体内研究：
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%).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)T1/2 (h)Cmax (ng/mL) CL (mL/min/kg)F (%)
1 (i.v.)17.2
10 (p.o.)2.6299576.81%
体外研究：
PI3K/mTOR Inhibitor-11 (compound 8o) inhibits various human cancer cell lines HT29, HCT15, H3122, HeLa, SW620, and H446 viability with IC50 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.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备