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编 号：F756658
分子式：C27H27F2N9O4S
分子量：611.62
分子式：C27H27F2N9O4S
分子量：611.62
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CAS No: 2891692-83-2
产品详情
生物活性：
PI3K/mTOR Inhibitor-12 is a potent, orally active and selective PI3K/mTOR inhibitor with IC50 values of 0.06 nM and 3.12 nM for PI3Kα and mTOR, respectively. PI3K/mTOR Inhibitor-12 has antitumor activity. PI3K/mTOR Inhibitor-12 has lower liver toxicity.
体内研究：
PI3K/mTOR Inhibitor-12 (compound 48; 20 mg/kg; p.o.; daily, for 14 d) inhibits tumor growth of HCT116 xenografts in female BALB/c nude mice.PI3K/mTOR Inhibitor-12 (1 and 5 mg/kg; i.v. and p.o.; male SD rats) has fast plasma clearance (1428 mL/h/kg) and short T1/2 (2.33 h) and the AUC0-∞ is 1356 h*ng/mL.Animal Model:HCT116 xenografts in female BALB/c nude mice
Dosage:20 mg/kg
Administration:Oral administration, daily, for 14 days
Result:Reduced the growth of HCT116 tumors, and the tumor growth inhibition (TGI) was 73.33%.Had lower liver toxicity of HCT116 xenografts in female BALB/c nude mice.
Animal Model:Male SD rats
Dosage:1 and 5 mg/kg
Administration:Intravenous injection (1 mg/kg) and oral administration (5 mg/kg)
Result:1.19ParameterI.V. (1 mg/kg)ParameterP.O. (5 mg/kg)
T1/2 (h)0.6T1/2 (h)2.33
CL (mL/h/kg)1428Cmax (ng/mL)1218
Vdss (mL/Kg)528AUC0-∞ (h*ng/mL)1356
AUC0-∞ (h*ng/mL)760F%33.1
体外研究：
PI3K/mTOR Inhibitor-12 (compound 48; 72 h) inhibits cancer cells growth with IC50 values of 0.07, 0.09, 0.54, 0.54, and 0.68 μM for PC-3, HT-29,HCT116, LOVO, and HUVEC cells, respectively.PI3K/mTOR Inhibitor-12 (0.25-1 μM; 12-48 h; HCT116 and HT-29 cells) inhibits the activation of PI3K and mTOR in the cellular context.
PI3K/mTOR Inhibitor-12 is a potent, orally active and selective PI3K/mTOR inhibitor with IC50 values of 0.06 nM and 3.12 nM for PI3Kα and mTOR, respectively. PI3K/mTOR Inhibitor-12 has antitumor activity. PI3K/mTOR Inhibitor-12 has lower liver toxicity.
体内研究：
PI3K/mTOR Inhibitor-12 (compound 48; 20 mg/kg; p.o.; daily, for 14 d) inhibits tumor growth of HCT116 xenografts in female BALB/c nude mice.PI3K/mTOR Inhibitor-12 (1 and 5 mg/kg; i.v. and p.o.; male SD rats) has fast plasma clearance (1428 mL/h/kg) and short T1/2 (2.33 h) and the AUC0-∞ is 1356 h*ng/mL.Animal Model:HCT116 xenografts in female BALB/c nude mice
Dosage:20 mg/kg
Administration:Oral administration, daily, for 14 days
Result:Reduced the growth of HCT116 tumors, and the tumor growth inhibition (TGI) was 73.33%.Had lower liver toxicity of HCT116 xenografts in female BALB/c nude mice.
Animal Model:Male SD rats
Dosage:1 and 5 mg/kg
Administration:Intravenous injection (1 mg/kg) and oral administration (5 mg/kg)
Result:1.19ParameterI.V. (1 mg/kg)ParameterP.O. (5 mg/kg)
T1/2 (h)0.6T1/2 (h)2.33
CL (mL/h/kg)1428Cmax (ng/mL)1218
Vdss (mL/Kg)528AUC0-∞ (h*ng/mL)1356
AUC0-∞ (h*ng/mL)760F%33.1
体外研究：
PI3K/mTOR Inhibitor-12 (compound 48; 72 h) inhibits cancer cells growth with IC50 values of 0.07, 0.09, 0.54, 0.54, and 0.68 μM for PC-3, HT-29,HCT116, LOVO, and HUVEC cells, respectively.PI3K/mTOR Inhibitor-12 (0.25-1 μM; 12-48 h; HCT116 and HT-29 cells) inhibits the activation of PI3K and mTOR in the cellular context.
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