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SOS1-IN-14
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SOS1-IN-14图片
CAS NO:2793405-20-4
包装:10mg
市场价:8550元

产品介绍
SOS1-IN-14 是一种有效的、具有选择性和口服活性的 SOS1 抑制剂,IC50 值为 3.9 nM。SOS1-IN-14 可通过 P-糖蛋白介导的外排机制在肠道内被吸收。SOS1-IN-14 可用于研究 KRAS 突变的癌症。SOS1-IN-14 的抑瘤效果优于 BI-3406 。$
Cas No.2793405-20-4
分子式C29H29F3N6O2
分子量550.57
溶解度DMSO : 250 mg/mL (454.07 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

SOS1-IN-14 is a potent, selective and orally activeSOS1inhibitor with anIC50value 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 thanBI-3406[1].

SOS1-IN-14 (compound 13c) exhibits cellular SOS1 inhibition with an IC50of 21 nM[1].
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[1].

SOS1-IN-14 (50 mg/kg; p.o.; qd) exhibits 83.0% tumor suppression in Mia-paca-2 pancreas xenograft mice tumor models[1].
SOS1-IN-14 shows a favorable pharmacokinetic profile with a bioavailability of 86.8% in beagles[1].
Pharmacokinetic Parameters of SOS1-IN-14 (compound 13c) in ICR mice, Sprague-Dawley rats and Beagle dogs[1].

ICR MiceSprague-Dawley RatsBeagle 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)[1]
Dosage:50 mg/kg
Administration:p.o.; q.d., for 21 days
Result:Exhibited 83.0% tumor suppression.
Showed better potent tumor suppression thanBI-3406.

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