产品
编 号：F756025
分子式：C29H29F3N6O2
分子量：550.57
分子式：C29H29F3N6O2
分子量：550.57
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: 2793405-20-4
产品详情
生物活性：
SOS1-IN-14 is a potent, selective and orally active SOS1 inhibitor with an IC50 value of 3.9 nM. SOS1-IN-14 can be absorbed in the intestine via a P-glycoprotein-mediated efflux mechanism. SOS1-IN-14 can be used to research KRAS-mutated cancers. SOS1-IN-14 has better potent tumor suppression than BI-3406 (HY-125817).
体内研究：
SOS1-IN-14 (50 mg/kg; p.o.; qd) exhibits 83.0% tumor suppression in Mia-paca-2 pancreas xenograft mice tumor models.SOS1-IN-14 shows a favorable pharmacokinetic profile with a bioavailability of 86.8% in beagles.Pharmacokinetic Parameters of SOS1-IN-14 (compound 13c) in ICR mice, Sprague-Dawley rats and Beagle dogs.ICR Mice Sprague–Dawley Rats Beagle Dogs
Administrationp.o., 50 mg/kgi.v., 2 mg/kgp.o., 10 mg/kgi.v., 2 mg/kgp.o., 20 mg/kg
Tmax (h)0.50.0830.082
T1/2 (h)4.611.172.323.836.68
Cmax (μg/mL)267012612655681840
AUC0-24 (ng/mL·h)323009701683296225725
CL (mL/min/kg)/2068/11.3/
Vss (L/kg)/2126/3.88/
F (%)//34.5/86.8
Kel (h-1)0.265////
MRT (h)4.67////
Animal Model:BALB/c nude mice (KRAS G12C variant Mia-paca-2 xenograft models)
Dosage:50 mg/kg
Administration:p.o.; q.d., for 21 days
Result:Exhibited 83.0% tumor suppression.Showed better potent tumor suppression than BI-3406 (HY-125817).
体外研究：
SOS1-IN-14 (compound 13c) exhibits cellular SOS1 inhibition with an IC50 of 21 nM.SOS1-IN-14 has certain inhibition for CYP2D6, CYP2C9, CYP2C8 and CYP3A4 with IC50s of 2.5 μM, 6.5 μM, 43.3 μM and 54.3 μM, respectively, indicating that it has a certain risk of drug-drug interaction.
SOS1-IN-14 is a potent, selective and orally active SOS1 inhibitor with an IC50 value of 3.9 nM. SOS1-IN-14 can be absorbed in the intestine via a P-glycoprotein-mediated efflux mechanism. SOS1-IN-14 can be used to research KRAS-mutated cancers. SOS1-IN-14 has better potent tumor suppression than BI-3406 (HY-125817).
体内研究：
SOS1-IN-14 (50 mg/kg; p.o.; qd) exhibits 83.0% tumor suppression in Mia-paca-2 pancreas xenograft mice tumor models.SOS1-IN-14 shows a favorable pharmacokinetic profile with a bioavailability of 86.8% in beagles.Pharmacokinetic Parameters of SOS1-IN-14 (compound 13c) in ICR mice, Sprague-Dawley rats and Beagle dogs.ICR Mice Sprague–Dawley Rats Beagle Dogs
Administrationp.o., 50 mg/kgi.v., 2 mg/kgp.o., 10 mg/kgi.v., 2 mg/kgp.o., 20 mg/kg
Tmax (h)0.50.0830.082
T1/2 (h)4.611.172.323.836.68
Cmax (μg/mL)267012612655681840
AUC0-24 (ng/mL·h)323009701683296225725
CL (mL/min/kg)/2068/11.3/
Vss (L/kg)/2126/3.88/
F (%)//34.5/86.8
Kel (h-1)0.265////
MRT (h)4.67////
Animal Model:BALB/c nude mice (KRAS G12C variant Mia-paca-2 xenograft models)
Dosage:50 mg/kg
Administration:p.o.; q.d., for 21 days
Result:Exhibited 83.0% tumor suppression.Showed better potent tumor suppression than BI-3406 (HY-125817).
体外研究：
SOS1-IN-14 (compound 13c) exhibits cellular SOS1 inhibition with an IC50 of 21 nM.SOS1-IN-14 has certain inhibition for CYP2D6, CYP2C9, CYP2C8 and CYP3A4 with IC50s of 2.5 μM, 6.5 μM, 43.3 μM and 54.3 μM, respectively, indicating that it has a certain risk of drug-drug interaction.
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