化合物SSR128129E T6082

Product Introduction
Bioactivity


英文名: SSR128129E

描述: SSR128129E (SSR) 是一种变构和口服活性 FGFR1 抑制剂 (IC50:1.9 μM)，但不影响其他相关的 RTK。

细胞实验: 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)

激酶实验: 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.

体外活性: 在各种小鼠肿瘤模型中,SSR128129E（30 mg/kg,p.o.）可同时抑制原发性肿瘤的增殖和转移.在患有关节炎的小鼠中,SSR128129E（30 mg/kg,p.o.）抑制了炎症、血管生成和骨吸收,并缓解了临床症状.此外,SSR128129E对抗血管内皮细胞生长因子受体2顽固型肿瘤模型和敏感株的增殖有抑制作用,并增加抗血管内皮细胞生长因子受体2的抗肿瘤活性.

体内活性: 由于变构机制,SSR128129E在细胞实验中具有更强的活性。SSR128129剂量依赖性抑制FGF2-诱导的EC增殖和迁移（IC50：31/15.2 nM）。作为多靶点成纤维细胞生长因子受体抑制剂,SSR128129E抑制了FGFR1-4介导的反应,从而使多种细胞系的增殖和/或迁移被阻断,比如mPanc02,HEK-hFGFR2WT,PAE-hFGFR1,hB9-myeloma和人脐静脉内皮细胞株。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : 1 mg/mL (2.88 mM)
DMSO : 64 mg/mL (184.8 mM)


关键字: SSR-128129E | Fibroblast growth factor receptor | Inhibitor | SSR128129E | inhibit | FGFR

相关产品: SM27 | Mal-amido-PEG2-C2-amido-Ph-C2-CO-AZD | Dovitinib lactate hydrate | BO-264 | FGFR1 inhibitor-10 | S49076 HCl | FGFR3-IN-7 | S6K2-IN-1 | FGFR4-IN-4 | FIIN-4

相关库: Anti-Prostate Cancer Compound Library | Anti-Breast Cancer Compound Library | Anti-Cancer Compound Library | Angiogenesis related Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Kinase Inhibitor Library | Highly Selective Inhibitor Library | Tyrosine Kinase Inhibitor Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途