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SSR128129E free acid
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SSR128129E free acid图片
CAS NO:848463-13-8
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
SSR free acid
产品介绍
SSR128129E free acid 是口服可用的FGFR变构调节剂, 对FGFR1 的IC50值为1.9 μM。
生物活性

SSR128129E free acid is an orally available and allostericFGFRinhibitor with anIC50of 1.9 μM forFGFR1.

IC50& Target[1]

FGFR1

1.9 μM (IC50)

FGFR2

 

FGFR3

 

FGFR4

 

体外研究
(In Vitro)

SSR128129E inhibits FGF2-induced EC proliferation with an IC50of 31±1.6 nM, migration with an IC50of 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[1].

体内研究
(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[1].

分子量

324.33

Formula

C18H16N2O4

CAS 号

848463-13-8

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.