SSR128129E
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
SSR128129E是一种FGFR1的别构抑制剂,IC50值为1.9 μM[1].
成纤维细胞生长因子受体(FGFR)是成纤维细胞生长因子(FGF)的受体酪氨酸激酶,在癌症和炎症反应中扮演重要角色.FGF2在血管生成方面扮演重要角色[1][2].
SSR128129E是一种具有口服活性的FGFR1别构抑制剂.在人类脐静脉内皮细胞(HUVEC)中,SSR128129E可抑制FGF2诱导的内皮细胞(EC)增殖和迁移,IC50值分别为31和15.2 nM,并可抑制板状伪足形成.SSR128129E可抑制FGFR1-4介导的反应.在表达FGFR2的HEK293细胞中,SSR128129E可抑制FGF2诱导的FRS2和ERK1/2磷酸化[1].
在关节炎小鼠中,SSR128129E可抑制骨和关节损伤,并可减少发炎关节的血管生成.在原位Panc02肿瘤模型中,SSR128129E(30 mg/kg)可抑制44%的肿瘤生长.在小鼠4T1乳腺肿瘤中,SSR128129E(30 mg/kg)可减少40%的肿瘤重量和53%的肿瘤大小[1].在动脉粥样硬化易发的载脂蛋白E(apoE)缺陷小鼠中,SSR128129E(50 mg/kg)可减少内膜增生,并可减少FGFR2 mRNA水平和主动脉窦的病变大小[2].
参考文献：
[1]. Bono F, De Smet F, Herbert C, et al. Inhibition of tumor angiogenesis and growth by a small-molecule multi-FGF receptor blocker with allosteric properties. Cancer Cell, 2013, 23(4): 477-488.
[2]. Dol-Gleizes F, Delesque-Touchard N, Marès AM, et al. A new synthetic FGF receptor antagonist inhibits arteriosclerosis in a mouse vein graft model and atherosclerosis in apolipoprotein E-deficient mice. PLoS One, 2013, 8(11): e80027.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 346.31 |
| Cas No. | 848318-25-2 |
| Formula | C18H15N2O4·Na |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥17.3 mg/mL in DMSO |
| Chemical Name | sodium;2-amino-5-(1-methoxy-2-methylindolizine-3-carbonyl)benzoate |
| SDF | Download SDF |
| Canonical SMILES | CC1=C(N2C=CC=CC2=C1OC)C(=O)C3=CC(=C(C=C3)N)C(=O)[O-].[Na+] |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
质量控制和MSDS
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化学结构
