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SSR128129E

CAS No. : 848318-25-2

MCE 站：SSR128129E

产品活性：SSR128129E 是口服可用的 FGFR 变构调节剂， 对FGFR1 的 IC₅₀ 值为1.9 μM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：FGFR

In Vitro: SSR128129E inhibits FGF2-induced EC proliferation with an IC₅₀ of 31±1.6 nM, migration with an IC₅₀ of 15.2±4.5 nM, and lamellipodia formation in a dose dependent manner. SSR128129E inhibits responses mediated by FGFR1-4. For instance, SSR128129E blocks EC migration in response to FGF1, a ligand of FGFR1 and FGFR4, and capillary tube formation in response to FGF19, a ligand of FGFR4. Proliferation and migration of the murine pancreatic Panc02 tumor cell line in response to FGF7 are also blocked by SSR128129E, showing that SSR128129E inhibits FGFR subtypes of other species as well. SSR128129E blocks different FGFR subtypes in various cell lines with nanomolar potency.

In Vivo: Oral delivery of SSR128129E (30 mg/kg/day, from day 3) inhibits growth of orthotopic Panc02 tumors by 44% and delays growth of Lewis lung carcinoma. oral SSR128129E (30 mg/kg/day, from day 5) reduces tumor size and weight by 53% and 40%, respectively. SSR128129E inhibits the growth of subcutaneous CT26 colon tumors by 34% and of the multidrug resistant MCF7/ADR breast cancer xenograft model by 40%. SSR128129E reduces tumor invasiveness and metastasis of Panc02 tumor cells to peritoneal lymph nodes.

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