SSR128129E (SSR) is an allosteric and orally-active FGFR1 inhibitor (IC50: 1.9 μM), but not affecting other related RTKs.

FGFR1:1.9 μM

SSR128129E 可抑制 FGF2 诱导的 EC 增殖和迁移（IC50 =31 nM）和呈剂量依赖性地诱导纤毛形成。SSR128129E 可抑制由 FGFR1-4 介导的反应。例如，SSR128129E 可阻断心肌细胞对 FGF1（FGFR1 和 FGFR4 的配体）的迁移反应，以及对 FGF19（FGFR4 的配体）的毛细管形成反应。
SSR128129E能抑制鼠胰腺 Panc02 肿瘤细胞系由 FGF7 引起的增殖和迁移，这表明 SSR128129E 也能抑制其他物种的 FGFR 亚型。[1]

口服 SSR128129E 30 mg/kg/day，从第 3 天开始可抑制正位 Panc02 肿瘤生长 44%，并延缓 Lewis 肺癌的生长。从第 5 天开始可使肿瘤大小和重量分别减少 53% 和 40%。[1]
SSR128129E 可抑制皮下 CT26 结肠肿瘤生长，抑制耐多药 MCF7/ADR 乳腺癌异种移植模型生长。SSR128129E 可降低 Panc02 肿瘤细胞的侵袭性和向腹膜淋巴结的转移。[1]

Scintillation Proximity Assay, 125I-FGF-2 Binding: SPA protein A beads are supplied as a suspension in PBS at 20 mg/mL, then diluted with binding buffer (KCl, 400 mg/L; MgSO4 200 mg/L; NaCl 6.4 g/L; NaHCO3 3.7 g/L; NaH2PO4 0.141 mg/mL; bis Tris Propane 11.292 g/L; Glucose 4.5 g/L; Gelatin 0.1 %; pH 7.0) at 10 mg/mL. 125I-FGF-2 radioligand and FGFR-1IIIc? - Fc Chimera are diluted into binding buffer. Binding was performed on 96-well plates coated with 0.1 % gelatin. Total assay volume is 0.1 mL. Binding of 125I-FGF-2 is determined by incubation of SPA beads coated with protein A (0.5 mg/assay) with FGFR-1IIIc? - Fc chimera soluble receptor (5 ng/assay), FGF-2 (20 ng/assay) is used for non-specific binding determinations.

Cell proliferation of porcine aortic endothelial (PAE) and tumor cell lines is analyzed on exponentially growing cells that are starved for 16 hours in 0.2 % FBS containing medium and seeded at 4,000 cells/well in 96-well microplates. After exposure to mitogens and/or SSR for 72 hours, cell proliferation is assessed with the use of the CellTiter 96 AQueous One Solution Cell Proliferation Assay according to manufacturer’s instructions. 10 % FBS containing medium is used a positive control. (Only for Reference)