SOS1-IN-15

SOS1-IN-15 (Compound 37) is an orally active SOS1 inhibitor with an IC 50 of 5 nM. SOS1-IN-15 is a promising agent candidate for the research of KRAS-driven cancer In Vitro SOS1-IN-15 (Compound 37) (0.1 nM-0.1 mM; 72 h) displays prominent inhibitory activities in Mia-paca-2 cancer cells (IC 50 = 178 ± 42 nM). SOS1-IN-15 has a limited inhibition of CYP and hERG. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: Mia-paca-2 pancreas cancer cells Concentration: 0.1 nM-0.1 mM Incubation Time: 72 h Result: Inhibited the proliferation with an IC 50 of 178 ± 42 nM. In Vivo SOS1-IN-15 (Compound 37) (50 mg/kg; p.o.; daily for 22 days) inhibits tumor volume in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 Mice a T 1/2 (h) T max (h) C max (ng/mL) AUC (ng⋅h/mL) MRT (h) K el (h -1 ) SOS1-IN-15 11.4 3.67 1550 9900 4.19 0.25 a Compounds (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: T 1/2 , elimination half-life; T max , plasma peak time after administration; C max , maximum plasma concentration; AUC, area under concentration-time curve. MRT, mean residence time; K el , elimination rate constant. Form:Solid IC50& Target:SOS1 5 nM (IC 50 )

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