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My CartCAS：848318-25-2
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Light yellow to yellow Solid
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| CAS | 848318-25-2 |
| Name | SSR128129E |
| Molecular Formula | C18H15N2NaO4 |
| Molecular Weight | 346.31 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD25976751 |
| SMILES | O=C([O-])C1=CC(C(C2=C(C)C(OC)=C3C=CC=CN23)=O)=CC=C1N.[Na+] |
| Target Point | FGFR |
| Passage | Angiogenesis; Protein Tyrosine Kinase/RTK |
| Background | SSR128129E is an FGFR allosteric modulator. |
| Biological Activity | SSR128129E 是口服可用的 FGFR 变构调节剂， 对FGFR1 的 IC50 值为1.9 μM。[1] |
| In Vitro | SSR128129E抑制FGF2诱导的EC增殖，IC50为31±1.6nM，迁移IC50为15.2±4.5nM，并且以剂量依赖性方式形成片状伪足。 SSR128129E抑制由FGFR1-4介导的反应。例如，SSR128129E响应于FGF1(FGFR1和FGFR4的配体)以及响应于FGF19(FGFR4的配体)的毛细管形成而阻断EC迁移。响应于FGF7的鼠胰腺Panc02肿瘤细胞系的增殖和迁移也被SSR128129E阻断，表明SSR128129E也抑制其他物种的FGFR亚型。 SSR128129E阻断具有纳摩尔效力的各种细胞系中的不同FGFR亚型[1]。 |
| In Vivo | 口服递送SSR128129E(30mg/kg /天，从第3天开始)抑制原位Panc02肿瘤的生长44％并延迟Lewis肺癌的生长。口服SSR128129E(30mg/kg /天，从第5天开始)分别使肿瘤大小和重量减少53％和40％。 SSR128129E抑制皮下CT26结肠肿瘤生长34％，多药耐药MCF7/ADR乳腺癌异种移植模型生长40％。 SSR128129E可降低Panc02肿瘤细胞向腹膜淋巴结的侵袭和转移[1]。 |
| Cell Experiment | 从不同供体新鲜分离并在第2代和第5代之间使用的HUVEC在补充有20％胎牛血清(FBS)，2mM L-谷氨酰胺，30mg/L内皮细胞生长因子补充物(EGCS)的M199培养基中培养，10单位/ mL肝素和青霉素/链霉素。为了增殖，将EC在含有2％FBS的生长因子耗尽的M199培养基中饥饿过夜，并用含有SSR128129E或DMSO的10ng/mL bFGF刺激24小时。通过与1μCi/ mL [3H]胸苷[1]孵育，在最后2小时评估增殖。 |
| Animal Experiment | 小鼠：麻醉的BALB/c小鼠接种鼠4T1乳腺癌细胞。在肿瘤细胞接种后第5天随机分配肿瘤大小的肿瘤大小后，每天通过口服强饲法以30mg/kg的剂量给予SSR128129E或媒介物(0.6％甲基纤维素)，直到第21天实验结束。体积测量。在实验结束时，通过戊巴比妥注射处死小鼠，并解剖肺和肿瘤。使用解剖显微镜计数肺部可见的转移性结节[1]。 |
| Data Literature Source | [1]. Bono F，et al. Inhibition of tumor angiogenesis and growth by a small-molecule multi-FGF receptor blocker with allosteric properties. Cancer Cell. 2013 Apr 15;23(4):477-88. |
| Unit | Bottle |
| Specification | 5mg 10mM*1mL in DMSO 10mg |
SSR128129E 是 FGFR 变构调节剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
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