产品
编 号：F751496
分子式：C27H22FN3O6S
分子量：535.54
分子式：C27H22FN3O6S
分子量：535.54
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
结构图
CAS No: 2361215-32-7
产品详情
生物活性：
PI3K/mTOR Inhibitor-4 is an orally active pan-class I PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-4 has enzymatic inhibition activity for PI3Kα, PI3Kγ, PI3Kδ and mTOR with IC50 values of 0.63 nM, 22 nM, 9.2 nM and 13.85 nM, respectively. PI3K/mTOR Inhibitor-4 can be used for the research of cancer.
体内研究：
PI3K/mTOR Inhibitor-4 (compound 8d-1) (i.v., oral; 1mg/kg, 10 mg/kg) displays favorable pharmacokinetic parameters in Sprague?Dawley rats.PI3K/mTOR Inhibitor-4 (oral; 10-50 mg/kg) shows significant efficiency in Hela/A549 tumor xenograft models without causing significant weight loss and toxicity.Animal Model:SD rats (male; 200-220 g)
Dosage:1, 10 mg/kg
Administration:Intravenous, oral
Result:IV (1 mg/kg)PO (10 mg/kg)
CL (ml/min/kg)Vss (ml/kg)Tmax (h)Cmax (ng/ml)AUCinf (ng*h/ml)t1/2 (h)F(%)
8.61199.812.67886.674753.351.7824.1
Animal Model:BALB/c nude mice (female; 6-7 weeks; 18-22 g)
Dosage:10, 20, 40, 50 mg/kg/d (Hela model) and 20, 40 mg/kg/d (A549 model)
Administration:Oral
Result:Inhibited the growth of xenograft tumors in a dose-dependent manner.
体外研究：
PI3K/mTOR Inhibitor-4 (compound 8d-1) has enzymatic inhibition activity for PI3Kα, PI3Kδ, mTOR, PI3Kβ and PI3Kγ with IC50 values of 0.63 nM, 9.2 nM, 13.85 nM, 94.54 nM and 22 nM, respectively.PI3K/mTOR Inhibitor-4 shows potent anti-proliferation activity in A549, Hela, HCT-116, HepG2, A375 and MCF-7 cells with IC50 values of 1.35 nM, 1.22 nM, 13.44 nM, 1.08 nM, 18.4 nM and 8.26 nM, respectively.PI3K/mTOR Inhibitor-4 (2.5-10 μM; 24 h) inhibits the PI3K/AKT/mTOR pathway.
PI3K/mTOR Inhibitor-4 is an orally active pan-class I PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-4 has enzymatic inhibition activity for PI3Kα, PI3Kγ, PI3Kδ and mTOR with IC50 values of 0.63 nM, 22 nM, 9.2 nM and 13.85 nM, respectively. PI3K/mTOR Inhibitor-4 can be used for the research of cancer.
体内研究：
PI3K/mTOR Inhibitor-4 (compound 8d-1) (i.v., oral; 1mg/kg, 10 mg/kg) displays favorable pharmacokinetic parameters in Sprague?Dawley rats.PI3K/mTOR Inhibitor-4 (oral; 10-50 mg/kg) shows significant efficiency in Hela/A549 tumor xenograft models without causing significant weight loss and toxicity.Animal Model:SD rats (male; 200-220 g)
Dosage:1, 10 mg/kg
Administration:Intravenous, oral
Result:IV (1 mg/kg)PO (10 mg/kg)
CL (ml/min/kg)Vss (ml/kg)Tmax (h)Cmax (ng/ml)AUCinf (ng*h/ml)t1/2 (h)F(%)
8.61199.812.67886.674753.351.7824.1
Animal Model:BALB/c nude mice (female; 6-7 weeks; 18-22 g)
Dosage:10, 20, 40, 50 mg/kg/d (Hela model) and 20, 40 mg/kg/d (A549 model)
Administration:Oral
Result:Inhibited the growth of xenograft tumors in a dose-dependent manner.
体外研究：
PI3K/mTOR Inhibitor-4 (compound 8d-1) has enzymatic inhibition activity for PI3Kα, PI3Kδ, mTOR, PI3Kβ and PI3Kγ with IC50 values of 0.63 nM, 9.2 nM, 13.85 nM, 94.54 nM and 22 nM, respectively.PI3K/mTOR Inhibitor-4 shows potent anti-proliferation activity in A549, Hela, HCT-116, HepG2, A375 and MCF-7 cells with IC50 values of 1.35 nM, 1.22 nM, 13.44 nM, 1.08 nM, 18.4 nM and 8.26 nM, respectively.PI3K/mTOR Inhibitor-4 (2.5-10 μM; 24 h) inhibits the PI3K/AKT/mTOR pathway.
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