BGJ398
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mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
![Tyramine Signal Amplification (TSA)](/media/diy/images/page/figure2-01.png)
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
![Cell Counting Kit-8 (CCK-8)](/media/diy/images/page/CCK-8.jpg)
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
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SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
![Inhibitor Cocktails](/media/diy/images/page/Inhibitor Cocktails.jpg)
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
NVP-BGJ398是一种有效的、选择性的和可口服的FGFR酪氨酸激酶小分子抑制剂,分子式为C26H31Cl2N7O3,分子量为560。成纤维细胞生长因子受体1(FGFR1)、FGFR2、FGFR3和FGFR4是18种不同FGF配体的受体。这些配体-受体共同调节发育和正常生长控制期间的各种信号。BGJ398抑制癌细胞中细胞增殖,诱导细胞凋亡,并抑制异种移植模型中肿瘤的生长。
参考文献:
1. Fibroblast Growth Factor Receptors as Novel Therapeutic Targets in SNF5-Deleted Malignant Rhabdoid Tumors. S Wöhrle, A Weiss, M Ito, A Kauffmann, M Murakami. PLOS ONE. 2013
2. Rescue screens with secreted proteins reveal compensatory potential of receptor tyrosine kinases in driving cancer growth. F Harbinski, VJ Craig, S Sanghavi, D Jeffery, L Liu. Cancer Discovery, 2012
- 1. Ying Zhang, Qian Fang, et al. "Increased FGFR3 is involved in T-2 toxin-induced lesions of hypertrophic cartilage associated with endemic osteoarthritis." Hum Exp Toxicol. 2023 Jan-Dec:42:9603271231219480. PMID: 38059300
- 2. Longwei Hu, Yang Wang, et al. "Apoptosis repressor with caspase recruitment domain (ARC) promotes bone regeneration of bone marrow-derived mesenchymal stem cells by activating Fgf-2/PI3K/Akt signaling." Stem Cell Res Ther. 2021 Mar 16;12(1):185. PMID:33726822
- 3. Day EK, Sosale NG, et al. "Glioblastoma Cell Resistance to EGFR and MET Inhibition Can Be Overcome via Blockade of FGFR-SPRY2 Bypass Signaling." Cell Rep. 2020;30(10):3383-3396.e7. PMID:32160544
- 4. Serra M, Alysandratos KD, et al."Pluripotent stem cell differentiation reveals distinct developmental pathways regulating lung- versus thyroid-lineage specification." Development. 2017 Nov 1;144(21):3879-3893. PMID:28947536
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 560.48 |
Cas No. | 872511-34-7 |
Formula | C26H31Cl2N7O3 |
Synonyms | BGJ398,BGJ-398 |
Solubility | insoluble in H2O; insoluble in EtOH; ≥7 mg/mL in DMSO with gentle warming |
Chemical Name | 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-[6-[4-(4-ethylpiperazin-1-yl)anilino]pyrimidin-4-yl]-1-methylurea |
SDF | Download SDF |
Canonical SMILES | CCN1CCN(CC1)C2=CC=C(C=C2)NC3=CC(=NC=N3)N(C)C(=O)NC4=C(C(=CC(=C4Cl)OC)OC)Cl |
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。 |
细胞实验[1]: | |
细胞系 |
AN3CA、MFE296、MFE280、SNGM和HEC1A细胞 |
溶解方法 |
该化合物在DMSO中的溶解度小于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月 |
反应条件 |
0.5 μM,72 hours |
实验结果 |
与未处理的对照相比,使用抑制剂处理的AN3CA、MFE296和MFE280细胞阻滞在G0-G1的细胞比例显著增加,并且经历凋亡的细胞比例也显著增加。相比之下,NVP-BGJ398处理未改变FGFR2野生型子宫内膜癌细胞系SNGM或HEC1A的G0-G1阻滞的细胞百分比。此外,NVP-BGJ398处理对FGFR2野生型子宫内膜癌细胞系HEC1A中的凋亡没有影响。 |
动物实验[1]: | |
动物模型 |
AN3CA、MFE296、SNGM或HEC1A异种移植裸鼠 |
剂量 |
口服,30或50 mg/kg,每天 |
实验结果 |
NVP-BGJ398显著延迟了FGFR2突变的子宫内膜癌异种移植肿瘤的生长。相比之下,在FGFR2野生型子宫内膜癌细胞系SNGM的长期研究中,没有发现NVP-BGJ398的体内抑制效应,令人惊讶的是,通过延迟这些细胞中的肿瘤生长,确实观察到了在HEC1A细胞中的体内活性。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1] Konecny G E, Kolarova T, O'Brien N A, et al. Activity of the fibroblast growth factor receptor inhibitors dovitinib (TKI258) and NVP-BGJ398 in human endometrial cancer cells. Molecular cancer therapeutics, 2013, 12(5): 632-642. |
描述 | BGJ398 (NVP-BGJ398)是一种有效的和选择性的FGFR抑制剂,作用于FGFR1/2/3,IC50值为0.9 nM/1.4 nM/1 nM,对FGFR的选择性比FGFR4和VEGFR2高40倍以上,对Abl、Fyn、Kit、Lck、Lyn和Yes几乎没有作用。 | |||||
靶点 | FGFR1 | FGFR2 | FGFR3 | FGFR4 | ||
IC50 | 0.9 nM | 1.4 nM | 1 nM | 60 nM |
质量控制和MSDS
- 批次:
化学结构
![BGJ398](https://www.apexbt.com//media/diy/images/struct/A3014.png)
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