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SSR128129E free acid

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Catalog No. T13003Cas No. 848463-13-8
Alias SSR free acid

SSR128129E (free acid) is an orally available, allosteric inhibitor of FGFR, with an IC50 of 1.9 μM for FGFR1.

SSR128129E free acid

SSR128129E free acid

😃Good
Catalog No. T13003Alias SSR free acidCas No. 848463-13-8
SSR128129E (free acid) is an orally available, allosteric inhibitor of FGFR, with an IC50 of 1.9 μM for FGFR1.
Pack SizePriceAvailabilityQuantity
25 mg$1,5201-2 weeks
50 mg$1,9801-2 weeks
100 mg$2,5001-2 weeks
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Product Introduction

Bioactivity
Description
SSR128129E (free acid) is an orally available, allosteric inhibitor of FGFR, with an IC50 of 1.9 μM for FGFR1.
Targets&IC50
FGFR1:1.9 μM
In vitro
FGF2-induced EC proliferation(IC50 : 31±1.6 nM) inhibited by SSR128129E, 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. 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.
In vivo
Oral delivery of SSR128129E (30 mg/kg/day, from day 3) inhibits the growth of orthotopic Panc02 tumors by 44% and delays the growth of Lewis lung carcinoma. Administering SSR128129E orally (30 mg/kg/day, from day 5) reduces tumor size and weight by 53% and 40%, respectively. SSR128129E also inhibits the growth of subcutaneous CT26 colon tumors by 34% and the multidrug-resistant MCF7/ADR breast cancer xenograft model by 40%. Additionally, the compound reduces tumor invasiveness and metastasis of Panc02 tumor cells to peritoneal lymph nodes.
AliasSSR free acid
Chemical Properties
Molecular Weight324.33
FormulaC18H16N2O4
Cas No.848463-13-8
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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