产品
编 号：F756024
分子式：C28H27F3N6O2
分子量：536.55
分子式：C28H27F3N6O2
分子量：536.55
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
结构图
CAS No: 2793404-47-2
产品详情
生物活性：
SOS1-IN-15 (Compound 37) is an orally active SOS1 inhibitor with an IC50 of 5 nM. SOS1-IN-15 is a promising agent candidate for the research of KRAS-driven cancer.
体内研究：
SOS1-IN-15 (Compound 37) (50 mg/kg; p.o.; daily for 22 days) inhibits tumor volume in mice.Animal Model:BALB/c nude mice bearing Mia-paca-2 pancreas tumors
Dosage:50 mg/kg
Administration:Oral administration, daily for 22 days
Result:Showed 49% tumor inhibition. No animal mortality and significant difference in the mice’s body weight were observed during the study period.
Animal Model:Male CD-1 Mice
Dosage:20 mg/kg
Administration:Oral administration (Pharmacokinetic Analysis)
Result:In Vivo Pharmacokinetic Properties of the Compounds in Male CD-1 MiceaT1/2 (h) Tmax (h) Cmax (ng/mL) AUC (ng?h/mL) MRT (h) Kel (h-1)
SOS1-IN-1511.43.67155099004.190.25
aCompounds (20 mg/kg) were P.O. dosed in a mixture of 63% water + 30% PEG +5 % DMSO + 2% Tween 80 in male ICR mice (n = 3). Abbreviations: T1/2, elimination half-life; Tmax, plasma peak time after administration; Cmax, maximum plasma concentration; AUC, area under concentration-time curve. MRT, mean residence time; Kel, elimination rate constant.
体外研究：
SOS1-IN-15 (Compound 37) (0.1 nM-0.1 mM; 72 h) displays prominent inhibitory activities in Mia-paca-2 cancer cells (IC50 = 178 ± 42 nM).SOS1-IN-15 has a limited inhibition of CYP and hERG.
SOS1-IN-15 (Compound 37) is an orally active SOS1 inhibitor with an IC50 of 5 nM. SOS1-IN-15 is a promising agent candidate for the research of KRAS-driven cancer.
体内研究：
SOS1-IN-15 (Compound 37) (50 mg/kg; p.o.; daily for 22 days) inhibits tumor volume in mice.Animal Model:BALB/c nude mice bearing Mia-paca-2 pancreas tumors
Dosage:50 mg/kg
Administration:Oral administration, daily for 22 days
Result:Showed 49% tumor inhibition. No animal mortality and significant difference in the mice’s body weight were observed during the study period.
Animal Model:Male CD-1 Mice
Dosage:20 mg/kg
Administration:Oral administration (Pharmacokinetic Analysis)
Result:In Vivo Pharmacokinetic Properties of the Compounds in Male CD-1 MiceaT1/2 (h) Tmax (h) Cmax (ng/mL) AUC (ng?h/mL) MRT (h) Kel (h-1)
SOS1-IN-1511.43.67155099004.190.25
aCompounds (20 mg/kg) were P.O. dosed in a mixture of 63% water + 30% PEG +5 % DMSO + 2% Tween 80 in male ICR mice (n = 3). Abbreviations: T1/2, elimination half-life; Tmax, plasma peak time after administration; Cmax, maximum plasma concentration; AUC, area under concentration-time curve. MRT, mean residence time; Kel, elimination rate constant.
体外研究：
SOS1-IN-15 (Compound 37) (0.1 nM-0.1 mM; 72 h) displays prominent inhibitory activities in Mia-paca-2 cancer cells (IC50 = 178 ± 42 nM).SOS1-IN-15 has a limited inhibition of CYP and hERG.
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