SOS1-IN-15

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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.

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.Cell Proliferation Assay 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 IC50 of 178 ± 42 nM.

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 tumorsDosage:50 mg/kg Administration:Oral administration, daily for 22 daysResult: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).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: 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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MAPK/ERK Signaling

Raf

Raf

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2793404-47-2

536.548

C28H27F3N6O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 5 mg/mL (9.32 mM; 超声助溶 (<60°C)

C(=O)(C1(C#N)CC1)N2C[C@]3(N(CC2)C=4C(OC3)=CC=5C(C4)=C(N[C@H](C)C6=C(F)C(C(F)F)=CC=C6)N=C(C)N5)[H]

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(-20℃)

With Ice Pack

≥ 2 years