SOS1-IN-15 (Compound 37) 是一种具有口服活性的SOS1抑制剂，IC50为 5 nM。SOS1-IN-15 可用于 KRAS 驱动型癌症研究。
| 生物活性 | SOS1-IN-15 (Compound 37) is an orally activeSOS1inhibitor with anIC50of 5 nM. SOS1-IN-15 is a promising drug candidate for the research of KRAS-drivencancer[1]. |
| IC50& Target[1] | |
体外研究
(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 (IC50= 178 ± 42 nM)[1].
SOS1-IN-15 has a limited inhibition of CYP and hERG[1].
Cell Proliferation Assay[1] | Cell Line: | Mia-paca-2 pancreas cancer cells | | Concentration: | 0.1 nM-0.1 mM | | Incubation Time: | 72 h | | Result: | Inhibited the proliferation with an IC50of 178 ± 42 nM. |
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体内研究
(In Vivo) | SOS1-IN-15 (Compound 37) (50 mg/kg; p.o.; daily for 22 days) inhibits tumor volume in mice[1].
| Animal Model: | BALB/c nude mice bearing Mia-paca-2 pancreas tumors[1] | | 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[1] | | Dosage: | 20 mg/kg | | Administration: | Oral administration (Pharmacokinetic Analysis) | | Result: | In Vivo Pharmacokinetic Properties of the Compounds in Male CD-1 Micea
| T1/2(h) | Tmax(h) | Cmax(ng/mL) | AUC (ng·h/mL) | MRT (h) | Kel(h-1) | | SOS1-IN-15 | 11.4 | 3.67 | 1550 | 9900 | 4.19 | 0.25 |
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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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