UC-857993

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

一种鸟嘌呤核苷酸交换因子 (GEF) 催化活性的小分子抑制剂，可与 SOS1 (Kd=14.7 uM) 结合并破坏 GEF-Ras 相互作用。

A small molecule inhibitor of guanine nucleotide exchange factor (GEF) catalytic activity that binds to SOS1 (Kd=14.7 uM) and disrupts GEF-Ras interaction; dose-dependently disrupts the SOS1-Ras interaction by competitively inhibiting the binding of SOS1cat to GDP-bound H-Ras in a microscale thermophoresis assay; dose-dependently inhibits Ras activation and downstream ERK activation mediated through EGFR-SOS1-Ras-Raf1-MEK-ERK signaling, specifically inhibits wild-type mouse embryonic fibroblast growth but not the growth of oncogenic H-Ras(G12V)-expressing mouse embryonic fibroblasts; inhibits Ras signaling and growth of pancreatic and prostate cancer cells.

Cell Proliferation Assay Cell Line:Mouse embryonic fibroblasts Concentration:0, 40, 60, and 80 μM Incubation Time:3 days Result:Selectively inhibited the growth of mouse fibroblasts, as exerting inhibition against wild-type mouse embryonic fibroblasts but not mouse embryonic fibroblasts expressing carcinogenic H-Ras(G12V).Western Blot AnalysisCell Line:NIH/3T3 cells Concentration:60 μM, 80 μM Incubation Time:2 hours; stimulated with 50 ng/ml EGF for 5 min Result:Inhibited EGF-induced the increase of the level of p-ERK and Ras-GTP.

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UC 857993 | UC857993

MAPK/ERK Signaling

Ras

Ras

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487001-04-7

403.906

C25H22ClNO2

>98% (HPLC)

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7-(2-chlorophenyl)-3b,6,6a,7,9,9a,10,12a-octahydrocyclopenta[4,5]pyrido[3,2,1-ij]cyclopenta[c]quinoline-2-carboxylic acid

(-20℃)

With Ice Pack

≥ 2 years